Ponatinib (AP24534) 化学構造
分子量: 532.56

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製品説明

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    Bcr-Abl製品生物活性の比較
  • 研究分野
  • Ponatinib (AP24534)のメカニズム

製品の説明

生物活性

製品説明 Ponatinib (AP24534) は、PI3KγとPI4KIIIβの新しくて強力な阻害剤で、IC50 がそれぞれ16 nM と 19 nMになる。
ターゲット Abl PDGFRα VEGFR2 FGFR1 Src
IC50 0.37 nM 1.1 nM 1.5 nM 2.2 nM 5.4 nM [1]
In vitro試験 AP24534 potently inhibits native Abl, AblT315I, and other clinically important Abl kinase domain mutants with IC50 of 0.30 nM–2 nM. AP24534 doesn't inhibit Aurora kinase family members, nor does it inhibit insulin receptor or CDK2/cyclin E. AP24534 inhibits proliferation of Ba/F3 cells expressing Bcr-Abl with IC50 of 0.5 nM, as well as Ba/F3 cells expressing a range of Bcr-Abl mutants with IC50 of 0.5 nM–36 nM. The inhibition of proliferation by AP24534 is correlated with induction of apoptosis. [1-2] In leukemic cell lines containing activated forms of FLT3, KIT, FGFR1, and PDGFRα receptors, AP24534 potently inhibits receptor phosphorylation and cellular proliferation with IC50 of 0.3 nM to 20 nM. In MV4-11 (FLT3-ITD(+/+)) but not RS4;11 (FLT3-ITD(–/–)) AML cells, AP24534 inhibits FLT3 signaling and induced apoptosis at less than 10 nM. AP24534 inhibits viability of primary leukemic blasts from a FLT3-ITD positive AML patient with IC50 of 4 nM but not those from patients with AML expressing native FLT3. [3] In Ba/F3 cells engineered to express activated FGFR1-4, AP24534 potently inhibits FGFR-mediated signaling and viability with IC50 lower than 40 nM. In cell lines representing multiple tumor types (endometrial, bladder, gastric, breast, lung, and colon), and containing FGFRs dysregulated by a variety of mechanisms, AP24534 inhibits FGFR-mediated signaling with IC50 less than 40 nM and inhibits cell growth with IC50 of 7 nM–181 nM. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
EoL-1-cell M{nGRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Lne2lEPTB;MD6wNFAxODByM{W5JO69VQ>? MkDKV2FPT0WU
MV-4-11 M2\uN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwMECwNFk2PiEQvF2= NHzwVHVUSU6JRWK=
MEG-01 NH22OldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXFTWM2OD1yLkCwNFEzQCEQvF2= MnK3V2FPT0WU
LAMA-84 NVXNU2RGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPHNHZGUUN3ME2wMlAxODF4NTFOwG0> NXLzcZpLW0GQR1XS
CGTH-W-1 NUnyT2ZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fDU2lEPTB;MD6wNFE3QSEQvF2= NYnRRmJnW0GQR1XS
KASUMI-1 NV24eJQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLMTWM2OD1yLkCwNlE4KM7:TR?= NVXTZZpKW0GQR1XS
BE-13 NYTYe2xuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33HdmlEPTB;MD6wNFI2QSEQvF2= MnrtV2FPT0WU
CTV-1 NYq4cmNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwMEC1NlEh|ryP NVzCbZhYW0GQR1XS
NKM-1 NVrsfGdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q2b2lEPTB;MD6wNFY2PSEQvF2= M3nQN3NCVkeHUh?=
MONO-MAC-6 NF;XU4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjBZVdKSzVyPUCuNFA5OzdizszN Mmn3V2FPT0WU
A204 M2GzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4H6emlEPTB;MD6wNVIyQCEQvF2= NXvlbGlUW0GQR1XS
GDM-1 NFzNV5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TEfmlEPTB;MD6wNVg{OyEQvF2= MnjUV2FPT0WU
AN3-CA MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;wTWM2OD1yLkCxPFc{KM7:TR?= M3LLeXNCVkeHUh?=
BL-70 M{fHXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTBwMEKxPVkh|ryP MXLTRW5ITVJ?
Daudi MofQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLtS3ZKSzVyPUCuNFI2OzdizszN M{jRc3NCVkeHUh?=
KU812 MnfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;SfYNKSzVyPUCuNFI5PDhizszN NF;HXIpUSU6JRWK=
KG-1 NIjBd4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwMEOyPVQh|ryP NFPaRlVUSU6JRWK=
DOHH-2 NWj1eoFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HQbWlEPTB;MD6wOFgxOyEQvF2= NXq1VZBxW0GQR1XS
HuO9 Mn;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv4TWM2OD1yLkC1OFQ5KM7:TR?= NHPKd|NUSU6JRWK=
EB2 M4LEOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX5TWM2OD1yLkC1OVc3KM7:TR?= NF\heVBUSU6JRWK=
G-402 NYnG[mNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXDPHVKSzVyPUCuNFY{PDFizszN M2LrSXNCVkeHUh?=
SU-DHL-1 Ml\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwME[zO|kh|ryP NYjle5dMW0GQR1XS
NCI-H719 MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTOTWM2OD1yLkC3PFg5KM7:TR?= M2Gyb3NCVkeHUh?=
MLMA MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXkTWM2OD1yLkC5NFYh|ryP MVLTRW5ITVJ?
KM12 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrnc2RKSzVyPUCuNFk4OzdizszN NGrld2FUSU6JRWK=
SUP-T1 MmXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnEVFBjUUN3ME2wMlA6QTh{IN88US=> MlftV2FPT0WU
MZ1-PC NVPZVldYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVWwcW0zUUN3ME2wMlEyOzN4IN88US=> NVS1R3cxW0GQR1XS
MFE-296 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDxWpI1UUN3ME2wMlEyQDN7IN88US=> M173OnNCVkeHUh?=
ALL-PO MkSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPqXI1KSzVyPUCuNVI1PDNizszN MmHIV2FPT0WU
GB-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f0cWlEPTB;MD6xNlUyOiEQvF2= MlHhV2FPT0WU
SIG-M5 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nXSWlEPTB;MD6xN|M4KM7:TR?= NWqyZXh4W0GQR1XS
P30-OHK MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3UNoNoUUN3ME2wMlE2Pjd{IN88US=> NGPob5VUSU6JRWK=
NCI-H716 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\4VmlEPTB;MD6xOlI3PiEQvF2= NXvy[Zh5W0GQR1XS
MPP-89 MkfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPOTW45UUN3ME2wMlE3QTN|IN88US=> M1nCPXNCVkeHUh?=
SF126 MlHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nBdWlEPTB;MD6xO|A3OyEQvF2= NXHle2FFW0GQR1XS
CTB-1 NGTnb2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLWSFJKSzVyPUCuNVc{OTZizszN M3fGTHNCVkeHUh?=
CA46 M1fYR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwMUe0PFkh|ryP Mk\DV2FPT0WU
NCI-H520 MlfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPFOGdKSzVyPUCuNVc4OzJizszN NIrTbVlUSU6JRWK=
CAL-85-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFS2UZpKSzVyPUCuNVc6OjdizszN NIH5Om5USU6JRWK=
NCI-H2342 M4\rbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInxZo9KSzVyPUCuNVg2PzdizszN MWDTRW5ITVJ?
697 NGjOVZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzTTWM2OD1yLkG4PFcyKM7:TR?= NWPR[Y0zW0GQR1XS
NY MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLXdHhYUUN3ME2wMlE6Ojh5IN88US=> NHTTWJJUSU6JRWK=
T98G MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLETWM2OD1yLkG5N|E5KM7:TR?= M2rudXNCVkeHUh?=
NCI-H1703 NWTXXI1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHFTWM2OD1yLkG5OlE2KM7:TR?= NFTkeWVUSU6JRWK=
NCI-H2087 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G3RWlEPTB;MD6yNFQ{QSEQvF2= NFHDXI1USU6JRWK=
PF-382 NIjweoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVS3fmR2UUN3ME2wMlIxQDd|IN88US=> MmPpV2FPT0WU
HCT-116 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLITWM2OD1yLkKxNFY6KM7:TR?= NEPTSlBUSU6JRWK=
CAKI-1 M3jtXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4W2fWlEPTB;MD6yNVY3PiEQvF2= Mn3LV2FPT0WU
CCF-STTG1 MlvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInUXodKSzVyPUCuNlI1PzVizszN MlTVV2FPT0WU
D-392MG NV7qc4pOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDWTWM2OD1yLkKzNVc4KM7:TR?= M4naU3NCVkeHUh?=
RT-112 M3rjSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HsOWlEPTB;MD6yN|c6PSEQvF2= NYLuW4ttW0GQR1XS
MES-SA NEKz[ZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMkSxPFch|ryP MofMV2FPT0WU
LC-2-ad Mm\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2C0RmlEPTB;MD6yOFI3PSEQvF2= M{nQdnNCVkeHUh?=
NOS-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3YTWM2OD1yLkK0N|Y4KM7:TR?= M2LT[XNCVkeHUh?=
NALM-6 NWm2S4JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\IWpVXUUN3ME2wMlI2PTR|IN88US=> MUXTRW5ITVJ?
TE-15 NVjYZmxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPhRYFKSzVyPUCuNlYxQTFizszN NIDXVoJUSU6JRWK=
786-0 MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXmTWM2OD1yLkK2NlI5KM7:TR?= MmHTV2FPT0WU
IST-MES1 NUnwTpdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PkVGlEPTB;MD6yOlgzQSEQvF2= M3HFe3NCVkeHUh?=
KYSE-180 MmLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\LTWM2OD1yLkK2PFkyKM7:TR?= M2[2dXNCVkeHUh?=
YT M4HBUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLTTWM2OD1yLkK2PVc1KM7:TR?= NE\6S2xUSU6JRWK=
A427 MkHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmW3TWM2OD1yLkK3NlY1KM7:TR?= MVLTRW5ITVJ?
KYSE-450 MmXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnZZWM1UUN3ME2wMlI4OzJ7IN88US=> M2nMTXNCVkeHUh?=
HuH-7 NIricoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwMke3OlMh|ryP MVXTRW5ITVJ?
CAS-1 M{jJeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rBXGlEPTB;MD6yPFMxOyEQvF2= MofQV2FPT0WU
KURAMOCHI NFnoNVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwMki0NVkh|ryP M1zvcnNCVkeHUh?=
ACHN MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\wR3VKSzVyPUCuNlk{OjNizszN MlyzV2FPT0WU
HGC-27 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPQS|dKSzVyPUCuNlk{PTNizszN MUPTRW5ITVJ?
A172 NWLlUm5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37OVmlEPTB;MD6yPVU4PyEQvF2= NEWyRnBUSU6JRWK=
SNU-449 NHTkOldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTBwMkm5OlQh|ryP MkDTV2FPT0WU
SW982 NV7TPXhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrhTWM2OD1yLkK5PVc5KM7:TR?= MlW4V2FPT0WU
EFO-21 NE[yNoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG3NlBKSzVyPUCuN|A1OTFizszN NWnqbJV{W0GQR1XS
NCI-H2030 NXrsbWp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLRd4FKSzVyPUCuN|EyPjRizszN MUTTRW5ITVJ?
HT-144 NYTC[3VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHm1bnhKSzVyPUCuN|EzQCEQvF2= NET3dldUSU6JRWK=
MFE-280 M1HkV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwM{G0OVMh|ryP M2\zOnNCVkeHUh?=
SK-LU-1 MmrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfXfGl3UUN3ME2wMlMyPDZ4IN88US=> NGr6[ldUSU6JRWK=
NCI-H2052 NIjqZVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwM{G0PFQh|ryP NXn0U2U4W0GQR1XS
SK-HEP-1 MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwM{OzOlgh|ryP NFvOOYNUSU6JRWK=
QIMR-WIL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF72ZY5KSzVyPUCuN|M1OjRizszN MoHhV2FPT0WU
A2780 M3vKVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXQVmVKSzVyPUCuN|Q{ODRizszN MXTTRW5ITVJ?
ACN MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwM{S4O|Mh|ryP NH:w[5JUSU6JRWK=
BxPC-3 NU[wXGsyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPDTWM2OD1yLkO0PVg6KM7:TR?= Mk\CV2FPT0WU
BCPAP NWXMPGx3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorDTWM2OD1yLkO2NFAyKM7:TR?= M2TnenNCVkeHUh?=
HOP-62 M17wUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4noOGlEPTB;MD6zOlExPiEQvF2= NVP3R2p{W0GQR1XS
SW1710 NGDEW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrwTWM2OD1yLkO2OFU2KM7:TR?= MmXOV2FPT0WU
OPM-2 M1HQeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DuPWlEPTB;MD6zOlQ4OyEQvF2= NYXNTYxHW0GQR1XS
DBTRG-05MG NW\ZTmZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwM{iwOVQh|ryP NV3HXWdOW0GQR1XS
SK-MEL-24 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwM{m3PVEh|ryP MlXlV2FPT0WU
8305C MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TXSGlEPTB;MD6zPVc6OyEQvF2= M3LyS3NCVkeHUh?=
OVCAR-4 NFXrXVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r6[mlEPTB;MD60NVU5PiEQvF2= MnrxV2FPT0WU
HLE MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrwOGFKSzVyPUCuOFE5PiEQvF2= MkLVV2FPT0WU
NCI-H747 NYXOVow1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLmTWM2OD1yLkSyNVM4KM7:TR?= MXjTRW5ITVJ?
SW780 NHLHZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXDcJdyUUN3ME2wMlQzOzR4IN88US=> M2nDWnNCVkeHUh?=
KYSE-150 NEjTXohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLQTWM2OD1yLkSyOFE2KM7:TR?= NVjGPWFyW0GQR1XS
H4 NF3KRXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7RcIx3UUN3ME2wMlQzPDVzIN88US=> M{TMVHNCVkeHUh?=
SW1088 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTBwNESzPUDPxE1? M3Lqd3NCVkeHUh?=
SF268 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTBwNES4OkDPxE1? M{TsbXNCVkeHUh?=
RT4 NUHMNHJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2T2Z2lEPTB;MD60OVEyOSEQvF2= M1zLWHNCVkeHUh?=
NCI-H522 NIDVTnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjVUXVKSzVyPUCuOFUzPyEQvF2= M1;xcnNCVkeHUh?=
LCLC-97TM1 M{HJPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITCOnhKSzVyPUCuOFYyQTVizszN NIj2PHdUSU6JRWK=
CAL-39 NYPWb3ZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzGOoxKSzVyPUCuOFY2OTlizszN M1viU3NCVkeHUh?=
CAL-120 M3XLd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\wZplCUUN3ME2wMlQ4PjR|IN88US=> M3PQcnNCVkeHUh?=
ESS-1 M4C5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm2[FRKSzVyPUCuOFc5OjFizszN MXvTRW5ITVJ?
KARPAS-45 NYm5fpFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTBwNEi5N|Mh|ryP NUTm[FFYW0GQR1XS
DU-4475 MkHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7GNmJtUUN3ME2wMlQ6PTFzIN88US=> MoXsV2FPT0WU
VMRC-RCZ NUjnPXJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\sT2tRUUN3ME2wMlQ6QTB2IN88US=> MojSV2FPT0WU
HOS NHnWcI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTBwNUCzOlUh|ryP MXLTRW5ITVJ?
MOLT-16 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTuO2RKSzVyPUCuOVE5ODhizszN M124eXNCVkeHUh?=
RPMI-6666 NH3JVIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwNUKxN|Uh|ryP NYnMW2NDW0GQR1XS
K052 NVHr[Y1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLDV3l6UUN3ME2wMlUzOTRizszN NVTDfXV[W0GQR1XS
EHEB NXPzWFhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M376XGlEPTB;MD61NlE5OiEQvF2= MWTTRW5ITVJ?
MFH-ino MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwNUKzOVEh|ryP MmmwV2FPT0WU
A4-Fuk NWHmWopPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrnTWM2OD1yLkWyOVI5KM7:TR?= M3PaTnNCVkeHUh?=
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SK-MEL-3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfYepVUUUN3ME2xMlY{QTB{IN88US=> MnfRV2FPT0WU
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L-428 Mny5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TOeGlEPTB;MT65PVE4QSEQvF2= NH;nXpdUSU6JRWK=
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MC-IXC Mo\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XCNmlEPTB;Mj6wNlI4OyEQvF2= NHr6VnlUSU6JRWK=
COLO-678 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\jSVlKSzVyPUKuNFQzODdizszN NXfK[4R6W0GQR1XS
MEL-JUSO M1\SXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jse2lEPTB;Mj6wO|g2OSEQvF2= MlTaV2FPT0WU
HCC38 NIjIdmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJwMEi0N|Mh|ryP M1fGWnNCVkeHUh?=
UACC-62 NWPCOXZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL3NVFKSzVyPUKuNFg5PTVizszN NHTuO5NUSU6JRWK=
OAW-42 MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f2bWlEPTB;Mj6wPVcyOSEQvF2= MVHTRW5ITVJ?
LB996-RCC MonPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\XeVdDUUN3ME2yMlE{QDF5IN88US=> NGHLbFVUSU6JRWK=
COR-L105 NIHqcphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjJdnl3UUN3ME2yMlE3Ozd|IN88US=> NFLyPGVUSU6JRWK=
RCC10RGB NYXENJNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;xVo9nUUN3ME2yMlE5PTd4IN88US=> NVHLb2NCW0GQR1XS
A431 NUT0ZXFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTJwMUmwNVkh|ryP MVTTRW5ITVJ?
NCI-H292 NUC1dZg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWK2S2c2UUN3ME2yMlI{QTVzIN88US=> NWm0UoZYW0GQR1XS
SK-UT-1 NFu5NlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJwM{OxPFQh|ryP M2X2TnNCVkeHUh?=
PANC-08-13 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjHSYxKSzVyPUKuN|MzOzVizszN NEW1[IdUSU6JRWK=
ST486 MnWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojzTWM2OD1{LkSxNFQ5KM7:TR?= MULTRW5ITVJ?
SJSA-1 NX\kUlg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7YTWM2OD1{LkSxNlcyKM7:TR?= NFK4eJRUSU6JRWK=
RKO NGi4eWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXFTWM2OD1{LkSyNFI6KM7:TR?= MWnTRW5ITVJ?
NCI-H1793 MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TFV2lEPTB;Mj60OFAzQSEQvF2= NV\nTpZrW0GQR1XS
639-V MmTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvwTWM2OD1{LkS1N|gzKM7:TR?= MWjTRW5ITVJ?
ES3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzZTWM2OD1{LkS5O|M4KM7:TR?= M4\0R3NCVkeHUh?=
NCI-H1792 NIfCWJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTJwNU[4NlYh|ryP MlPmV2FPT0WU
NCI-H1651 NX:yZ3V5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TySmlEPTB;Mj61PFIyKM7:TR?= MXzTRW5ITVJ?
SN12C MnzuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFm4OXVKSzVyPUKuOVg1QDdizszN NHuxbnZUSU6JRWK=
COLO-679 NUDiO5dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVniZplMUUN3ME2yMlU5PjB3IN88US=> MULTRW5ITVJ?
U-118-MG NGTHcXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLIN|dKSzVyPUKuOVg5PzJizszN NUToVYF4W0GQR1XS
Ramos-2G6-4C10 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\jcZc3UUN3ME2yMlY1QDB5IN88US=> NIDmSZNUSU6JRWK=
HCT-15 NU\aU4NXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJwNki3PVIh|ryP NVXnbItUW0GQR1XS
MDA-MB-157 NFXTS|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJwN{C3OFch|ryP NYHRO4d5W0GQR1XS
K5 NWG3PZIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJwN{G4OFUh|ryP MY\TRW5ITVJ?
MKN45 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfkS2pKSzVyPUKuO|M{PjZizszN NHLHO|lUSU6JRWK=
DMS-273 NITZ[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTpcJU2UUN3ME2yMlc2PjN{IN88US=> NUDVWVNUW0GQR1XS
C8166 M1Pqbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7hTWM2OD1{Lke4OVE{KM7:TR?= MVrTRW5ITVJ?
Calu-3 NGK5RlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLyXIZKSzVyPUKuO|g6PjlizszN NUjCWmQxW0GQR1XS
SNB75 NHPGSZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJwOEi1N|Uh|ryP NXjxPWtPW0GQR1XS
BFTC-905 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTJwOUCxPVEh|ryP NXXCfGdrW0GQR1XS
C-4-II MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXycFdKSzVyPUKuPVE{PTNizszN M{PoZ3NCVkeHUh?=
MS-1 NIntNmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LuOGlEPTB;Mj65Olc3QSEQvF2= MWrTRW5ITVJ?
A375 NU\rSoIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDuTWM2OD1|LkC4NVg1KM7:TR?= MWHTRW5ITVJ?
KYSE-70 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLrTWM2OD1|LkC4PFgzKM7:TR?= NG\k[3VUSU6JRWK=
KYSE-510 NX;G[VlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXmTWM2OD1|LkGwPVk2KM7:TR?= M3\1TXNCVkeHUh?=
LN-405 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHYTWM2OD1|LkGzOVE5KM7:TR?= NYnRSIVqW0GQR1XS
BOKU MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnkcnQ{UUN3ME2zMlE1OjV4IN88US=> MX\TRW5ITVJ?
TE-10 NGqyblJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjwOpptUUN3ME2zMlE4OzZ{IN88US=> MUnTRW5ITVJ?
MKN1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTNwMUi0PFMh|ryP MkfXV2FPT0WU
M059J NFzwV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTNwMkCxO|Mh|ryP MoTGV2FPT0WU
GOTO NETVcoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTNwMkKwN|kh|ryP M3rsRnNCVkeHUh?=
DK-MG MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTNwMkW5O|Yh|ryP NGTLV2VUSU6JRWK=
NCI-H727 MkfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDESFRKSzVyPUOuNlY2QCEQvF2= MX7TRW5ITVJ?
NB12 M{DVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT4TWM2OD1|LkOzNlI1KM7:TR?= NGXtNZZUSU6JRWK=
DOK NGfMZWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;tTWM2OD1|LkO2NVg3KM7:TR?= MXvTRW5ITVJ?
KYSE-410 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlm2TWM2OD1|LkO2Nlg4KM7:TR?= NHPyXGxUSU6JRWK=
AM-38 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DuTmlEPTB;Mz6zPFA2OSEQvF2= NXW5U5pQW0GQR1XS
GR-ST MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3T4R2lEPTB;Mz60OVc{OiEQvF2= NI[zPJJUSU6JRWK=
D-247MG NWj1dGZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzWTWM2OD1|LkS4NlY{KM7:TR?= M1vtUnNCVkeHUh?=
TE-8 M{LMeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS4NZBoUUN3ME2zMlQ6OzN|IN88US=> MX3TRW5ITVJ?
LS-411N MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nWVWlEPTB;Mz60PVY6OiEQvF2= M1LjSXNCVkeHUh?=
SK-MES-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1O1OWlEPTB;Mz61OlQ{OyEQvF2= MkfvV2FPT0WU
SF295 NVfJVYVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfVbFZnUUN3ME2zMlYyPTV{IN88US=> M{fWZXNCVkeHUh?=
SK-MEL-30 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4KzTGlEPTB;Mz62OVkzOSEQvF2= MlTEV2FPT0WU
LB2241-RCC M1HuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorqTWM2OD1|Lk[2NlYh|ryP MXPTRW5ITVJ?
PC-14 NYDJe2FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjtTWM2OD1|Lk[2OFM4KM7:TR?= NYPVcJBOW0GQR1XS
EW-7 NVz3UWpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTNwNke2PVMh|ryP MmXtV2FPT0WU
NMC-G1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofTTWM2OD1|LkexPFM4KM7:TR?= M2m0XXNCVkeHUh?=
TE-441-T MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXRSZJIUUN3ME2zMlc{ODJ6IN88US=> M3L2Z3NCVkeHUh?=
NCI-H1618 MlK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HQbmlEPTB;Mz64NVg4PSEQvF2= M4[xOnNCVkeHUh?=
PANC-03-27 MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWq3XFF3UUN3ME2zMlgyQTF4IN88US=> M2nOTXNCVkeHUh?=
NCI-H2228 NIfxU5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LkSGlEPTB;Mz64N|EzPiEQvF2= MVXTRW5ITVJ?
CAPAN-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fxTmlEPTB;Mz64O|AxQSEQvF2= NYjVeZJOW0GQR1XS
KLE NX7X[XBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTNwOUC2O{DPxE1? MnKyV2FPT0WU
Becker MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Wzd2lEPTB;Mz65Nlg1QSEQvF2= NFW5S5hUSU6JRWK=
SK-PN-DW MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DRV2lEPTB;ND6wO|k4PCEQvF2= NEfm[phUSU6JRWK=
Hs-578-T MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzyWZo5UUN3ME20MlA5OzB4IN88US=> M2HF[HNCVkeHUh?=
RS4-11 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jyW2lEPTB;ND6xNVI2PSEQvF2= NIDwfWlUSU6JRWK=
D-502MG NGjUdJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvDXoRKSzVyPUSuNVY6QTdizszN MX;TRW5ITVJ?
GI-1 M3X0XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoO2TWM2OD12LkK4Nlk6KM7:TR?= MofEV2FPT0WU
NCI-H209 MlXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLlTWM2OD12LkOzO|gh|ryP NH3MdJlUSU6JRWK=
SK-OV-3 M{Hnb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HjNWlEPTB;ND60PFE1QSEQvF2= NHe5eWlUSU6JRWK=
LOUCY MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHZRYk2UUN3ME20MlQ5PDN{IN88US=> NYTLfJRmW0GQR1XS
NCI-H69 NUC1XXB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTOZ5FKSzVyPUSuOVE4QTNizszN NYTwdnNlW0GQR1XS
SCC-9 NYO2cGc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW[4[3BvUUN3ME20MlU{OTd{IN88US=> NIXKVnZUSU6JRWK=
NCI-H526 MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTRwNUmyPVMh|ryP M1j3eXNCVkeHUh?=
NCI-H2170 NILJXZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPsTWM2OD12Lk[2O|cyKM7:TR?= Mon3V2FPT0WU
SR NHHSdVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLqenhKSzVyPUSuO|AxPDhizszN MoPjV2FPT0WU
CMK M1XHe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3L0WWlEPTB;ND63NlExOSEQvF2= M3u3VHNCVkeHUh?=
COLO-829 NX\ncYJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPzTWM2OD12Lke3NFQ{KM7:TR?= M3fZWnNCVkeHUh?=
HuO-3N1 M1q0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTRwOEOyPFEh|ryP MnrkV2FPT0WU
5637 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIm1PIpKSzVyPUSuPVA1QDdizszN MkHkV2FPT0WU
A253 NEnMZ4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFWwd5dKSzVyPUSuPVc4ODhizszN MWnTRW5ITVJ?
NB10 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3IV2RKSzVyPUWuNFc1QTdizszN NV\CbGRwW0GQR1XS
SF539 NGTIcmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\0TWM2OD13LkC5PVU6KM7:TR?= M3fxT3NCVkeHUh?=
HAL-01 MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTVwMUS2OFUh|ryP MW\TRW5ITVJ?
MHH-ES-1 NH\US2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\ITWM2OD13LkG2PVI2KM7:TR?= MmTHV2FPT0WU
DEL M{C4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETpSY9KSzVyPUWuNlc2QDJizszN NHnWbWRUSU6JRWK=
NCI-H1299 MkC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTXTWM2OD13LkO1NFA4KM7:TR?= NXfBOJJ{W0GQR1XS
ChaGo-K-1 NY\pdXRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVewV2hoUUN3ME21MlM2OTB5IN88US=> MUTTRW5ITVJ?
HMV-II MmD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTpVpdkUUN3ME21MlM6PDNizszN NEm0eYxUSU6JRWK=
NB69 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml2xTWM2OD13LkO5OlMyKM7:TR?= M3OxXXNCVkeHUh?=
NCI-H1882 NX;ZbYNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPG[m5KSzVyPUWuOFM{PjRizszN MliwV2FPT0WU
SNU-475 M3XP[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVuzeo9uUUN3ME21MlQ4OTdzIN88US=> NGezOm9USU6JRWK=
RXF393 MoTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u2SmlEPTB;NT60PFQ6PCEQvF2= NGPWXohUSU6JRWK=
CAL-51 NVLEWJAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T2cWlEPTB;NT62Nlg2OyEQvF2= MV;TRW5ITVJ?
SW1573 NYq3T5pvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGG4OJdKSzVyPUWuOlM2OzRizszN MlXVV2FPT0WU
GCT Mk\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TQXmlEPTB;NT63OVkzQSEQvF2= M{jzUnNCVkeHUh?=
COR-L88 M{mzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O4dGlEPTB;NT63Olg1PiEQvF2= MkXBV2FPT0WU
MDA-MB-134-VI M3ntfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTBb3BKSzVyPUWuPFc2OzZizszN MXrTRW5ITVJ?
NB5 NHPSfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jpSGlEPTB;NT65NlQ1KM7:TR?= NULIfGpYW0GQR1XS
GMS-10 M1HSWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfuTWM2OD13Lkm2PFYyKM7:TR?= NYXofW1EW0GQR1XS
CHP-212 M2fnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnriTWM2OD14LkS4NlY4KM7:TR?= Mmj1V2FPT0WU
TE-11 NX\FPZZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTZwNUWxPFIh|ryP NVjnSZMzW0GQR1XS
SW962 NETiVm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M165Z2lEPTB;Nj62OVc4PCEQvF2= NFiyOFVUSU6JRWK=
MZ2-MEL MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;4bJhIUUN3ME22MlgzODFzIN88US=> NIPve5hUSU6JRWK=
C-33-A NFXvTohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTZwOUG2PFgh|ryP NXjv[WM2W0GQR1XS
IGR-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTZwOUe4NlYh|ryP MXXTRW5ITVJ?
MOLT-4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\vNFVKSzVyPUeuNVU1ODZizszN M1O3S3NCVkeHUh?=
NCI-H1650 M3PUNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Kzc2lEPTB;Nz6yO|A1PiEQvF2= MlvqV2FPT0WU
AsPC-1 NXfjNHFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPkSo1mUUN3ME23MlI5PjB3IN88US=> MlXpV2FPT0WU
SNU-C2B MlPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvWOFNKSzVyPUeuNlk2PzFizszN NUjvUGs1W0GQR1XS
MKN7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTdwM{eyN|Uh|ryP NFL4[HFUSU6JRWK=
SW620 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjZc2FKSzVyPUeuN|gzODVizszN M4[wfXNCVkeHUh?=
SK-MEL-28 M{faeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTdwNEC3PVgh|ryP Mn3PV2FPT0WU
TE-6 NELGXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\6clA1UUN3ME23MlQ1QTB6IN88US=> MWTTRW5ITVJ?
D-263MG MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTdwNEW3OlIh|ryP M1;TWnNCVkeHUh?=
NCI-H1355 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XjbWlEPTB;Nz63O|AzQSEQvF2= M4XC[XNCVkeHUh?=
DSH1 NEe1THhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrGTWM2OD15Lke5O|YzKM7:TR?= MlzyV2FPT0WU
NCI-H460 NEK5UnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXQTWM2OD16LkCwOlk1KM7:TR?= NUDNNZBuW0GQR1XS
NCI-H1563 NVrqdHVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjKd4x3UUN3ME24MlA4PTB6IN88US=> MmTBV2FPT0WU
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CAL-72 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;4TWM2OD1zOT62O|M4KM7:TR?= MlnrV2FPT0WU
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U251 M{fuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfPTWM2OD1{ND6wOlY5KM7:TR?= NULZdm9FW0GQR1XS
LoVo MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJ2LkmyPFIh|ryP NWXJdXhkW0GQR1XS
GCIY M17kbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr4TWM2OD1{NT6yPFc4KM7:TR?= NYfOcHZ5W0GQR1XS
NUGC-3 NELVemNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PtVWlEPTB;MkWuN|MyPiEQvF2= NEK5OZlUSU6JRWK=
LNCaP-Clone-FGC NEDGfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HQRmlEPTB;MkWuN|Q6QCEQvF2= Mlf1V2FPT0WU
PA-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDrRnBTUUN3ME2yOU43QDN|IN88US=> MoKzV2FPT0WU
OE33 NUjBO2s{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LGVmlEPTB;MkWuOlg2OyEQvF2= NVTQcXliW0GQR1XS
HT-29 NV\WU2NjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJ3Lke4O|kh|ryP NEPwUY1USU6JRWK=
RCM-1 NVTueoJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXWVHZQUUN3ME2yOU46PjV4IN88US=> M{jXPXNCVkeHUh?=
NCI-H1522 NGD0cWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPXXllmUUN3ME2yOU46QTFzIN88US=> Mn\hV2FPT0WU
LB373-MEL-D MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLqTWM2OD1{Nj6xO|A5KM7:TR?= MVnTRW5ITVJ?
NCI-H1436 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[0T2xKSzVyPUK2MlI4OzhizszN M1TOUHNCVkeHUh?=
COLO-824 MofKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37nOmlEPTB;Mk[uOFAxOiEQvF2= NGXMSFBUSU6JRWK=
CP50-MEL-B MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rxSWlEPTB;Mk[uOVY4PSEQvF2= MmnhV2FPT0WU
EGI-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7OSWxKSzVyPUK3MlI3QThizszN Mnq1V2FPT0WU
LAN-6 NHvPZ5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ5LkO1PVgh|ryP Mkj6V2FPT0WU
GAK MoDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTJ5LkSyNlUh|ryP NGPQSWdUSU6JRWK=
MDA-MB-175-VII MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXvR5h[UUN3ME2yO{42ODV|IN88US=> M2GxTnNCVkeHUh?=
JVM-2 NFHsW3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2f4TWlEPTB;MkeuOlYzOiEQvF2= MmnKV2FPT0WU
UACC-257 MkDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLxVZhKSzVyPUK3MlY5PzhizszN MUDTRW5ITVJ?
SW1783 M4\wTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjsSmFuUUN3ME2yO{44Pzh|IN88US=> NEXaN2lUSU6JRWK=
HT-3 NI\xVWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2S5V2lEPTB;MkiuNlE3PiEQvF2= MnzQV2FPT0WU
RL NHyxTmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTo[pRKSzVyPUK4MlU6OTFizszN NEfITFlUSU6JRWK=
TK10 M1vyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2D5WWlEPTB;MkiuOlU{PSEQvF2= MXrTRW5ITVJ?
HT55 M1u0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NET5R4RKSzVyPUK5MlA2PjVizszN NEHTVVhUSU6JRWK=
BT-20 MmDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrE[VNKSzVyPUK5MlA2QDZizszN MW\TRW5ITVJ?
TGBC24TKB Mne1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T0T2lEPTB;MkmuNVg{OSEQvF2= Mnf0V2FPT0WU
HSC-2 NE[yd2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\HTWM2OD1{OT6zNFAyKM7:TR?= NF3uU45USU6JRWK=
COLO-205 NEDRd5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFn5S25KSzVyPUK5MlM6PDRizszN M1W4XnNCVkeHUh?=
GT3TKB MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fUdWlEPTB;MkmuOlg4PyEQvF2= MWjTRW5ITVJ?
T47D NVS2WYJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTiTWM2OD1{OT64OVgzKM7:TR?= NFu3bY9USU6JRWK=
OMC-1 NV:4VVBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkezTWM2OD1|MD6xPVE6KM7:TR?= NV\l[JFqW0GQR1XS
PFSK-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHiOItKSzVyPUOxMlI3PTlizszN NUHUZ5NJW0GQR1XS
JEG-3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XYb2lEPTB;M{GuN|U3OSEQvF2= M{ThenNCVkeHUh?=
RD NVrRNIFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLTfY5TUUN3ME2zNU42OTF3IN88US=> MnXOV2FPT0WU
NCI-H64 MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoK5TWM2OD1|Mj60NVc6KM7:TR?= MYHTRW5ITVJ?
DMS-114 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTN{LkSxPFIh|ryP MnLiV2FPT0WU
NCI-H661 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITKOVhKSzVyPUOyMlY2ODFizszN NH7D[ItUSU6JRWK=
CAL-148 M2PWfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXPTWM2OD1|Mj62OlY2KM7:TR?= NYOz[lNmW0GQR1XS
HuP-T3 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\LSnpSUUN3ME2zNk46OzN6IN88US=> NVrrW2ExW0GQR1XS
ES4 MmXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrSTplKSzVyPUOzMlE4ODVizszN NXvTdmE1W0GQR1XS
Ca9-22 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrv[IpHUUN3ME2zN{41PjBzIN88US=> MofmV2FPT0WU
LP-1 NXPvfHZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUT6Z2s1UUN3ME2zOE4xQSEQvF2= MWPTRW5ITVJ?
AU565 NEX0d29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLyRlZKSzVyPUO0MlUxPjlizszN NXP1OIJGW0GQR1XS
MDA-MB-453 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonYTWM2OD1|NT6xOFI3KM7:TR?= NEW0cFRUSU6JRWK=
SNU-C1 MlLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ezfWlEPTB;M{WuNVcyKM7:TR?= NUHYdW1kW0GQR1XS
SW13 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrxTWM2OD1|NT60NFc3KM7:TR?= MnTFV2FPT0WU
NCI-H2122 M4TP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojzTWM2OD1|NT61OVk5KM7:TR?= NUDRTGpbW0GQR1XS
NCI-H1395 M2nVNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NICySIJKSzVyPUO1MlY3QTFizszN M{LQVnNCVkeHUh?=
J-RT3-T3-5 NITqcXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTN4LkCyPVQh|ryP MYLTRW5ITVJ?
COR-L279 MkK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXP6dJpqUUN3ME2zOk4yQThzIN88US=> M3G2[HNCVkeHUh?=
ATN-1 NEHre3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\OPVRZUUN3ME2zOk45PTF4IN88US=> MmPpV2FPT0WU
HCC2998 NICy[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTN4Lki1O|Eh|ryP NIT3UI5USU6JRWK=
UM-UC-3 MkfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DRXWlEPTB;M{[uPFY4PSEQvF2= M2fZcnNCVkeHUh?=
DV-90 MljSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnS1TWM2OD1|Nj65NFY4KM7:TR?= NVra[ml{W0GQR1XS
ES8 NVG3fppQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PDTGlEPTB;M{[uPVMyQCEQvF2= NF\mZ3BUSU6JRWK=
YAPC MlPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfzTWM2OD1|Nj65OlU1KM7:TR?= NGLXWYFUSU6JRWK=
HCC1599 NEfZSFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTN5LkG2NVgh|ryP MmPKV2FPT0WU
UMC-11 M3rzSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTN5LkK1NFMh|ryP M1vVdXNCVkeHUh?=
THP-1 NHHKb41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3H0U2lEPTB;M{euNlg3QCEQvF2= M1u2dHNCVkeHUh?=
OCUB-M MlHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzGTpVKSzVyPUO3MlI5QTFizszN Mk[3V2FPT0WU
NCI-H1693 NFjPUWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXkOmQzUUN3ME2zO{4{OjN|IN88US=> MmToV2FPT0WU
NCI-H345 Ml\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTN5LkO2NlQh|ryP M{nVS3NCVkeHUh?=
COLO-800 NHnEOW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXSWmQ1UUN3ME2zO{42PjdizszN NUnRU5NYW0GQR1XS
COLO-320-HSR MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTZTWM2OD1|OD6zOFkzKM7:TR?= NH:zb|hUSU6JRWK=
NCI-H596 M4nNc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\WdFlKSzVyPUO4MlQ1QDlizszN MWDTRW5ITVJ?
NCI-H187 NV7qdGdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz6TWM2OD1|OD63N|Q1KM7:TR?= M{PUNXNCVkeHUh?=
ECC4 M3HtNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTCTWM2OD1|OT6wPFE1KM7:TR?= MoXlV2FPT0WU
KP-4 NG\GOINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzwfXVKSzVyPUO5MlEzOzVizszN Moq1V2FPT0WU
NCI-H2227 NEHOfHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HZd2lEPTB;M{muN|k1QSEQvF2= M2fUcHNCVkeHUh?=
22RV1 M4nEeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1joeWlEPTB;M{muPFM6QCEQvF2= MVLTRW5ITVJ?
SAS MmjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[1RmdHUUN3ME20NE4xQTZizszN M1vveXNCVkeHUh?=
PANC-10-05 M{HMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1frdGlEPTB;NECuNVgzQCEQvF2= MUTTRW5ITVJ?
MDA-MB-468 M{\ROmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTRyLkWzOFYh|ryP MXfTRW5ITVJ?
RPMI-7951 Mki5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjDe2RKSzVyPUSxMlIxPzVizszN NGHS[ZpUSU6JRWK=
BB49-HNC M{X0[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTRzLkKxO|kh|ryP NE\zZ2tUSU6JRWK=
23132-87 NYTJWVdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTRzLkK3N|Ih|ryP NVWzSoZZW0GQR1XS
HCC1569 NGfCUXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTaWVVKSzVyPUSxMlI5QDVizszN M4OyTnNCVkeHUh?=
CP66-MEL MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jSW2lEPTB;NEKuNVg5PiEQvF2= NVrlfGl4W0GQR1XS
K-562 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTR{LkK4OVQh|ryP NYf5cIZOW0GQR1XS
OCI-AML2 NYe0SlJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTPTWM2OD12Mj64PVc1KM7:TR?= MUjTRW5ITVJ?
SW756 NIDNXYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTqSFl2UUN3ME20N{4xOzh6IN88US=> MYTTRW5ITVJ?
M14 M3y1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jMV2lEPTB;NEOuN|E5QSEQvF2= M3zJenNCVkeHUh?=
NCI-H1623 NWfy[HhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXY[HlKSzVyPUSzMlQ3PCEQvF2= MVXTRW5ITVJ?
KNS-81-FD Mlj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jJNWlEPTB;NEOuO|YzKM7:TR?= NG[4[IFUSU6JRWK=
TGBC1TKB NUfOW5NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojHTWM2OD12Mz65NFk6KM7:TR?= NHXhXlVUSU6JRWK=
RERF-LC-MS Ml3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{f2e2lEPTB;NEOuPVI5OSEQvF2= MnvuV2FPT0WU
PC-3 NYDkW5VFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnEWGdKSzVyPUS0MlQ{PDdizszN M1\0cHNCVkeHUh?=
HuP-T4 NYXrNYVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrmeXhHUUN3ME20OE41PDd2IN88US=> MWLTRW5ITVJ?
NCI-H510A M2\x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrQWJlKSzVyPUS0MlcxQCEQvF2= NFTqN5lUSU6JRWK=
LB2518-MEL Ml7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXH6eXM4UUN3ME20OE44QTN5IN88US=> M2TzN3NCVkeHUh?=
TE-5 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjQWlNKSzVyPUS1Mlk2QDFizszN MY\TRW5ITVJ?
EW-24 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\IU2lFUUN3ME20Ok4yPzJ|IN88US=> MlqzV2FPT0WU
LB647-SCLC NGjqXYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TBeGlEPTB;NE[uNlE2PSEQvF2= M1LwS3NCVkeHUh?=
NCI-H524 M{PuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTwTWM2OD12Nj63NVg2KM7:TR?= NH\OU3hUSU6JRWK=
EW-11 M1;qPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTR4LkmzO|Mh|ryP NX3iW|M1W0GQR1XS
KALS-1 NUXCbm86T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\oS2lEPTB;NEeuNlA3PiEQvF2= MWXTRW5ITVJ?
BT-474 MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHhTWM2OD12Nz60NlE3KM7:TR?= M1niO3NCVkeHUh?=
SK-N-AS MlGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LhbWlEPTB;NEeuPFg5KM7:TR?= NEDaVoJUSU6JRWK=
HCC2157 NInhUFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnYdXhKSzVyPUS4MlA4PiEQvF2= NH;uXYxUSU6JRWK=
HCC1954 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Xv[2lEPTB;NEiuNVcxPCEQvF2= M{P0b3NCVkeHUh?=
FADU NVG3dVVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTR6LkOwN|Eh|ryP MXjTRW5ITVJ?
S-117 NFm2[|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2K1cmlEPTB;NEiuN|gyPSEQvF2= MYLTRW5ITVJ?
LS-1034 NHvsZYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUGwRohCUUN3ME20PE44ODZ5IN88US=> MljuV2FPT0WU
CAMA-1 NVzZOYVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHSyU29KSzVyPUS5MlU2PDNizszN NFLqdYRUSU6JRWK=
LU-134-A MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTR7LkiwPFUh|ryP MX3TRW5ITVJ?
NCI-H1838 NYPOcpdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTR7LkiwPFch|ryP NXz4NYNJW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo試験 In a mouse xenograft model of Ba/F3 cells expressing native Bcr-Abl, AP24534 (2.5 mg/kg and 5 mg/kg) prolongs mice median survival. In the xenograft model of Ba/F3 Bcr-AblT315I, AP24534 (10 mg/kg–50 mg/kg) significantly suppresses tumor growth. AP24534 (30 mg/kg) decreases the phosphorylated Bcr-Abl and phosphorylated CrkL levels in the tumors. [2]
臨床試験 AP24534 is currently under Phase II clinical trials in treatment with leukemia.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Peptide substrate phosphorylation assays with GST-Abl kinase domains The effect of AP24534 (0-320 nM) on GST-Abl kinase activity is assessed by using a synthetic peptide substrate (Abltide: EAIYAAPFAKKK). Assays are carried out at 30 °C for 15 min in 25 μL reaction mixture: 8 mM MOPS (pH 7), 0.2 mM EDTA, 50 μM Abltide, 30 mM MgCl2, 10 mM β-glycerol phosphate, 1 mM EGTA, 0.002% Brij-35, 0.4 mM DTT, 0.2 mg/mL BSA, 0.4 mM sodium orthovanadate, 10 nM WT or mutant GST-Abl kinase, and 100 µM ATP/γ-32[P]ATP (5000 cpm/pmol). Reactions are terminated by transferring a portion of the reaction mixture onto a p81 phosphocellulose filter and immersing in 0.75% phosphoric acid. Filters are washed 3 times in 0.75% phosphoric acid, rinsed in acetone, and air dried; phosphate incorporation is determined by scintillation counting. All results are corrected for background binding to the filters, as determined by omitting peptide substrate from the kinase reaction. Time course experiments to establish the linear range of enzymatic activity precedes kinase assays.

細胞アッセイ: [2]

細胞株 Ba/F3 cells expressing Bcr-Abl or a range of single mutations in the kinase domain of Bcr-Abl
濃度 0-625 nM
反応時間 72 hours
実験の流れ Ba/F3 cell lines are distributed in 96-well plates (4 × 103 cells/well) and incubated with AP24534 for 72 hours. Proliferation is measured using a methanethiosulfonate (MTS)-based viability assay (CellTiter96 Aqueous One Solution). All values are normalized to the control wells with no drug. IC50 values are reported as the mean of three independent experiments performed in quadruplicat

動物実験: [1]

動物モデル Mouse xenograft models of Ba/F3 cells expressing Bcr-Abl or Bcr-AblT315I
製剤 Dissolved in 25 mM citrate buffer, pH 2.75
投薬量 2.5 mg/kg and 5 mg/kg for Ba/F3 Bcr-Abl; 2.5 mg/kg–50 mg/kg for Ba/F3 Bcr-AblT315I
投与方法 Oral gavage once daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Ponatinib (AP24534) SDF
分子量 532.56
化学式

C29H27F3N6O

CAS No. 943319-70-8
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 30 mg/mL (56.33 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 10 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-(2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide

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Source Cancer Cell, 2012, 22(5), 656-667 . Ponatinib (AP24534) purchased from Selleck
Method Western blot
Cell Lines RCH-ACV cells
Concentrations 50 nM
Incubation Time 1-24 h
Results Treatment of these cells with a CSK inhibitor (BMS-599626) or a BTK inhibitor (PCI-32765) did not recapitulate the dasatinib/ponatinib phenotype.

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Source , , Genome Biol, 2014, 15(8): 428 . Ponatinib (AP24534) purchased from Selleck
Method Cell Proliferation Assay
Cell Lines KatoIII cells
Concentrations 0-0.5 nM
Incubation Time
Results Each of the inhibitors demonstrated a statistically significant lower IC50 in FGFR2-amplified KatoIII cells compared to non-FGFR2-amplified AGS cells at all concentrations tested.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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