Ponatinib (AP24534) 化学構造
分子量: 532.56

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Quality Control & MSDS

製品説明

  • Compare Bcr-Abl Inhibitors
    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 NUT6Z3c1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojQTWM2OD1yLkCwNFAxODB|NUmg{txO MojDV2FPT0WU
MV-4-11 NWrhXlQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwMECwNFk2PiEQvF2= MV;TRW5ITVJ?
MEG-01 MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nNS2lEPTB;MD6wNFAyOjhizszN MYHTRW5ITVJ?
LAMA-84 Ml3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3NfHBKSzVyPUCuNFAxOTZ3IN88US=> NXe5ZnU4W0GQR1XS
CGTH-W-1 NWnOZohvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;jTWM2OD1yLkCwNVY6KM7:TR?= M13vd3NCVkeHUh?=
KASUMI-1 NGG1eW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETYfGhKSzVyPUCuNFAzOTdizszN NWfye5FIW0GQR1XS
BE-13 M3LhOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjsW3gxUUN3ME2wMlAxOjV7IN88US=> Mln4V2FPT0WU
CTV-1 MlXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPST2FKSzVyPUCuNFA2OjFizszN NF3qNVBUSU6JRWK=
NKM-1 NEO0dHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTBwMEC2OVUh|ryP MXvTRW5ITVJ?
MONO-MAC-6 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nOc2lEPTB;MD6wNFg{PyEQvF2= NXe4cnJtW0GQR1XS
A204 M2Dye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LQSmlEPTB;MD6wNVIyQCEQvF2= NILaXnpUSU6JRWK=
GDM-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH6eJNKSzVyPUCuNFE5OzNizszN M2HscXNCVkeHUh?=
AN3-CA Ml\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTTTWM2OD1yLkCxPFc{KM7:TR?= MX7TRW5ITVJ?
BL-70 M2j4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknpTWM2OD1yLkCyNVk6KM7:TR?= MWnTRW5ITVJ?
Daudi NX\CSZFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7UWnhKSzVyPUCuNFI2OzdizszN MofPV2FPT0WU
KU812 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwMEK4OFgh|ryP NX7lXVd{W0GQR1XS
KG-1 NWrWZ4FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zvSGlEPTB;MD6wN|I6PCEQvF2= Mnr5V2FPT0WU
DOHH-2 NYL3bZdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrMTWM2OD1yLkC0PFA{KM7:TR?= NV\Fb3FzW0GQR1XS
HuO9 Ml7nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33jcWlEPTB;MD6wOVQ1QCEQvF2= NWryfJBwW0GQR1XS
EB2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwMEW1O|Yh|ryP MkjsV2FPT0WU
G-402 NV;3doFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwME[zOFEh|ryP M1u5[HNCVkeHUh?=
SU-DHL-1 NW[2cW9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS5cVlKSzVyPUCuNFY{PzlizszN NU\WbFJIW0GQR1XS
NCI-H719 MmjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDvcpVKSzVyPUCuNFc5QDhizszN NXTBR5A5W0GQR1XS
MLMA M4rVUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwMEmwOkDPxE1? M372fnNCVkeHUh?=
KM12 MkXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfKd5Z6UUN3ME2wMlA6PzN5IN88US=> Moi5V2FPT0WU
SUP-T1 Ml:yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T6NGlEPTB;MD6wPVk5OiEQvF2= M2HPe3NCVkeHUh?=
MZ1-PC MmTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\FTWM2OD1yLkGxN|M3KM7:TR?= MWjTRW5ITVJ?
MFE-296 M1\BPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fVS2lEPTB;MD6xNVg{QSEQvF2= NETBfIdUSU6JRWK=
ALL-PO M2XYbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\TS4dKSzVyPUCuNVI1PDNizszN NUDuSpFoW0GQR1XS
GB-1 MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTjTWM2OD1yLkGyOVEzKM7:TR?= M33LfHNCVkeHUh?=
SIG-M5 MoPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTBwMUOzO{DPxE1? MWTTRW5ITVJ?
P30-OHK M4TQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG0TWM2OD1yLkG1OlczKM7:TR?= M2nsO3NCVkeHUh?=
NCI-H716 NI\CXWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHh[21KSzVyPUCuNVYzPjZizszN MnuyV2FPT0WU
MPP-89 MlzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwMU[5N|Mh|ryP NF7me2xUSU6JRWK=
SF126 MnPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HDWmlEPTB;MD6xO|A3OyEQvF2= MnLRV2FPT0WU
CTB-1 M4O5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33sRmlEPTB;MD6xO|MyPiEQvF2= NXLleWdxW0GQR1XS
CA46 NVnr[pJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTlTWM2OD1yLkG3OFg6KM7:TR?= M2DJNXNCVkeHUh?=
NCI-H520 MnPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjKTHhmUUN3ME2wMlE4PzN{IN88US=> MVrTRW5ITVJ?
CAL-85-1 NYX0RWxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwMUe5Nlch|ryP MorEV2FPT0WU
NCI-H2342 MkKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K1TGlEPTB;MD6xPFU4PyEQvF2= NF7O[YFUSU6JRWK=
697 M1HCV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4X2OmlEPTB;MD6xPFg4OSEQvF2= M3nnVHNCVkeHUh?=
NY MmPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHGZohPUUN3ME2wMlE6Ojh5IN88US=> NXnTNJN[W0GQR1XS
T98G M1jJPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIezUYVKSzVyPUCuNVk{OThizszN NICyXZJUSU6JRWK=
NCI-H1703 NHXUV|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjmc|ZKSzVyPUCuNVk3OTVizszN NIrXdHFUSU6JRWK=
NCI-H2087 M2PZNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmGxTWM2OD1yLkKwOFM6KM7:TR?= Mn3NV2FPT0WU
PF-382 M{PDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwMkC4O|Mh|ryP MmLiV2FPT0WU
HCT-116 Mm[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fGe2lEPTB;MD6yNVA3QSEQvF2= NWHDNYtUW0GQR1XS
CAKI-1 MneyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLsXWtOUUN3ME2wMlIyPjZ4IN88US=> M1:yPHNCVkeHUh?=
CCF-STTG1 NVTXboF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XkSGlEPTB;MD6yNlQ4PSEQvF2= MmTDV2FPT0WU
D-392MG Mn24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnNTWM2OD1yLkKzNVc4KM7:TR?= MnfQV2FPT0WU
RT-112 MkLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzuTWM2OD1yLkKzO|k2KM7:TR?= M3mxNXNCVkeHUh?=
MES-SA MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTLfItKSzVyPUCuNlQyQDdizszN Mlr4V2FPT0WU
LC-2-ad M1Tpbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDHUXlNUUN3ME2wMlI1OjZ3IN88US=> NIKyOWlUSU6JRWK=
NOS-1 M2PQe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HQNGlEPTB;MD6yOFM3PyEQvF2= MkXlV2FPT0WU
NALM-6 MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFm4RWFKSzVyPUCuNlU2PDNizszN NF;V[lBUSU6JRWK=
TE-15 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHMTWM2OD1yLkK2NFkyKM7:TR?= NELCXmlUSU6JRWK=
786-0 MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELVWmlKSzVyPUCuNlYzOjhizszN MlfhV2FPT0WU
IST-MES1 NIrDWFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrBbmFiUUN3ME2wMlI3QDJ7IN88US=> NXGwUHJsW0GQR1XS
KYSE-180 Mm[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT0bYhKSzVyPUCuNlY5QTFizszN NEPDdXFUSU6JRWK=
YT MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwMk[5O|Qh|ryP NX7QTpdqW0GQR1XS
A427 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH61e2JKSzVyPUCuNlczPjRizszN M4jFOnNCVkeHUh?=
KYSE-450 MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwMkezNlkh|ryP M3jyVXNCVkeHUh?=
HuH-7 NVjkOYdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmP5TWM2OD1yLkK3O|Y{KM7:TR?= MUDTRW5ITVJ?
CAS-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTBwMkizNFMh|ryP NXi5V5h6W0GQR1XS
KURAMOCHI MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHETWM2OD1yLkK4OFE6KM7:TR?= MmfIV2FPT0WU
ACHN MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHvfoJNUUN3ME2wMlI6OzJ|IN88US=> NHLCbXdUSU6JRWK=
HGC-27 NWjCUXRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHhOphnUUN3ME2wMlI6OzV|IN88US=> MoXrV2FPT0WU
A172 M1WzUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjZW5Y5UUN3ME2wMlI6PTd5IN88US=> M3TPV3NCVkeHUh?=
SNU-449 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwMkm5OlQh|ryP NUW2PWlrW0GQR1XS
SW982 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zJZWlEPTB;MD6yPVk4QCEQvF2= MVTTRW5ITVJ?
EFO-21 NE\SO2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXSSYFKSzVyPUCuN|A1OTFizszN Mn7LV2FPT0WU
NCI-H2030 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfRWHdwUUN3ME2wMlMyOTZ2IN88US=> M3rMWHNCVkeHUh?=
HT-144 NISzTIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3OwU2lEPTB;MD6zNVI5KM7:TR?= NIDIWItUSU6JRWK=
MFE-280 M2i3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTBwM{G0OVMh|ryP NYjSSnVqW0GQR1XS
SK-LU-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDSVItMUUN3ME2wMlMyPDZ4IN88US=> NH:0R5hUSU6JRWK=
NCI-H2052 MoHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4OzWmlEPTB;MD6zNVQ5PCEQvF2= M1\JNnNCVkeHUh?=
SK-HEP-1 M1y5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DN[mlEPTB;MD6zN|M3QCEQvF2= MVHTRW5ITVJ?
QIMR-WIL M1Szbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\VOGJKSzVyPUCuN|M1OjRizszN M3jwTXNCVkeHUh?=
A2780 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHr3eG5KSzVyPUCuN|Q{ODRizszN NX;UN4hlW0GQR1XS
ACN MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL0TWM2OD1yLkO0PFc{KM7:TR?= NUPRfIhvW0GQR1XS
BxPC-3 MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLDS5JKSzVyPUCuN|Q6QDlizszN MWXTRW5ITVJ?
BCPAP NH7mcXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPFRnVWUUN3ME2wMlM3ODBzIN88US=> MYTTRW5ITVJ?
HOP-62 M4TwPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDRTWM2OD1yLkO2NVA3KM7:TR?= Ml;HV2FPT0WU
SW1710 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHuTWM2OD1yLkO2OFU2KM7:TR?= M3fDcnNCVkeHUh?=
OPM-2 M1LmRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnWTWM2OD1yLkO2OFc{KM7:TR?= M3vLXHNCVkeHUh?=
DBTRG-05MG NU\NOHhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3jTWM2OD1yLkO4NFU1KM7:TR?= NV7vVnpjW0GQR1XS
SK-MEL-24 MoGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrIWZVKSzVyPUCuN|k4QTFizszN MVLTRW5ITVJ?
8305C MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwM{m3PVMh|ryP MkH4V2FPT0WU
OVCAR-4 NHjVRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[2[mlEPTB;MD60NVU5PiEQvF2= NX7ob3pZW0GQR1XS
HLE M4S3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTBwNEG4OkDPxE1? NWjNVVZwW0GQR1XS
NCI-H747 NHzPcG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\qbWlEPTB;MD60NlE{PyEQvF2= NGPJSYpUSU6JRWK=
SW780 M12wSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPGcW1qUUN3ME2wMlQzOzR4IN88US=> MX3TRW5ITVJ?
KYSE-150 NYjvO5VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PrNWlEPTB;MD60NlQyPSEQvF2= MYDTRW5ITVJ?
H4 NVTodGc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnITWM2OD1yLkSyOFUyKM7:TR?= M3TUTHNCVkeHUh?=
SW1088 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwNESzPUDPxE1? MlzuV2FPT0WU
SF268 NYfn[3cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlqyTWM2OD1yLkS0PFYh|ryP MmfuV2FPT0WU
RT4 NFu0bZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTrTWM2OD1yLkS1NVEyKM7:TR?= NH3xZ5dUSU6JRWK=
NCI-H522 Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYraeItGUUN3ME2wMlQ2OjdizszN NIDCU4FUSU6JRWK=
LCLC-97TM1 M3zzSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\ZTWM2OD1yLkS2NVk2KM7:TR?= NEfjWFFUSU6JRWK=
CAL-39 M4O1c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfkdIRKSzVyPUCuOFY2OTlizszN M2X3R3NCVkeHUh?=
CAL-120 NFrHXphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwNEe2OFMh|ryP NHvjW5BUSU6JRWK=
ESS-1 NX\o[lMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rYdWlEPTB;MD60O|gzOSEQvF2= NYO2fVVwW0GQR1XS
KARPAS-45 M1ntT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3y1RmlEPTB;MD60PFk{OyEQvF2= M{nUT3NCVkeHUh?=
DU-4475 NUfQR2s3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPyTWM2OD1yLkS5OVEyKM7:TR?= MWjTRW5ITVJ?
VMRC-RCZ M3PS[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwNEm5NFQh|ryP MXnTRW5ITVJ?
HOS NHXVeHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTBwNUCzOlUh|ryP MkX2V2FPT0WU
MOLT-16 MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjMZ|JKSzVyPUCuOVE5ODhizszN M3LnPHNCVkeHUh?=
RPMI-6666 NHXVO5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmP3TWM2OD1yLkWyNVM2KM7:TR?= NWK1PIp4W0GQR1XS
K052 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPNTWM2OD1yLkWyNVQh|ryP NIrqSpVUSU6JRWK=
EHEB M1TVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jMUmlEPTB;MD61NlE5OiEQvF2= MXPTRW5ITVJ?
MFH-ino NFi3[nlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmOyTWM2OD1yLkWyN|UyKM7:TR?= Ml7IV2FPT0WU
A4-Fuk NH76VGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHaTWM2OD1yLkWyOVI5KM7:TR?= M{DtdnNCVkeHUh?=
SW1417 NFXzV2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfsOG5KSzVyPUCuOVI4QDFizszN NWr0W4lQW0GQR1XS
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TE-12 NWTlRVJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDMTWM2OD1yLkW1O|M2KM7:TR?= NFXhSWpUSU6JRWK=
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SIMA NUDVR2hET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LBWGlEPTB;MT60PFY5PyEQvF2= MYHTRW5ITVJ?
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KNS-42 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTFwOE[yOlYh|ryP MYHTRW5ITVJ?
NCI-H2452 NVPHPI5rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLGUWxoUUN3ME2xMlg6ODd2IN88US=> MnnDV2FPT0WU
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MC-IXC NW\jSnBTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj6SYJKSzVyPUKuNFIzPzNizszN NFfmXmFUSU6JRWK=
COLO-678 NF\IS49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJwMESyNFch|ryP MWDTRW5ITVJ?
MEL-JUSO M3vqdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4L5Z2lEPTB;Mj6wO|g2OSEQvF2= MUTTRW5ITVJ?
HCC38 NWrpWZdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTJwMEi0N|Mh|ryP MXrTRW5ITVJ?
UACC-62 NFfsZotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInBOmZKSzVyPUKuNFg5PTVizszN NF2z[VNUSU6JRWK=
OAW-42 M3zJPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYmwNmEzUUN3ME2yMlA6PzFzIN88US=> MnfxV2FPT0WU
LB996-RCC M3jNZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJwMUO4NVch|ryP NXfKWVVmW0GQR1XS
COR-L105 M4rQ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTJwMU[zO|Mh|ryP MlPGV2FPT0WU
RCC10RGB NW\5U4RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlezTWM2OD1{LkG4OVc3KM7:TR?= NV7IVHVLW0GQR1XS
A431 NYHUPZpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTJwMUmwNVkh|ryP NWr4NG46W0GQR1XS
NCI-H292 M{HpfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTlTWM2OD1{LkKzPVUyKM7:TR?= MoXtV2FPT0WU
SK-UT-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJwM{OxPFQh|ryP MXjTRW5ITVJ?
PANC-08-13 NIHNOIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVmyN3B{UUN3ME2yMlM{OjN3IN88US=> NUXYOGNKW0GQR1XS
ST486 NHvmT4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW2ZYNXUUN3ME2yMlQyODR6IN88US=> MnfDV2FPT0WU
SJSA-1 NEfrOotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfodJBKSzVyPUKuOFEzPzFizszN NYXNW3ZoW0GQR1XS
RKO NETWWWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnLTWM2OD1{LkSyNFI6KM7:TR?= MXHTRW5ITVJ?
NCI-H1793 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1OyXWlEPTB;Mj60OFAzQSEQvF2= M4PQOXNCVkeHUh?=
639-V MlruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJwNEWzPFIh|ryP NEDWb|dUSU6JRWK=
ES3 M1nJfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrnTWM2OD1{LkS5O|M4KM7:TR?= Mmn1V2FPT0WU
NCI-H1792 M1S2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\yVmlEPTB;Mj61OlgzPiEQvF2= M{jQV3NCVkeHUh?=
NCI-H1651 NVG4ZmozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJwNUiyNUDPxE1? NYXrbZZKW0GQR1XS
SN12C MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:wWoJmUUN3ME2yMlU5PDh5IN88US=> NWrDd5ZxW0GQR1XS
COLO-679 NX3KSHJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7QTWM2OD1{LkW4OlA2KM7:TR?= NU[0XpBXW0GQR1XS
U-118-MG MofQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvqfZJkUUN3ME2yMlU5QDd{IN88US=> NIfF[4tUSU6JRWK=
Ramos-2G6-4C10 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7RTWM2OD1{Lk[0PFA4KM7:TR?= M1nyWnNCVkeHUh?=
HCT-15 MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fP[GlEPTB;Mj62PFc6OiEQvF2= MnHTV2FPT0WU
MDA-MB-157 M{DERmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XNRmlEPTB;Mj63NFc1PyEQvF2= NHHBcWpUSU6JRWK=
K5 NHT1RWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHq5[GJKSzVyPUKuO|E5PDVizszN M3HsdnNCVkeHUh?=
MKN45 NGLjSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXzfolKSzVyPUKuO|M{PjZizszN NWPsTodtW0GQR1XS
DMS-273 NFewcXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HSWGlEPTB;Mj63OVY{OiEQvF2= NFjUUVhUSU6JRWK=
C8166 MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnjVGZzUUN3ME2yMlc5PTF|IN88US=> NH\tVpFUSU6JRWK=
Calu-3 MkjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXWwXnpkUUN3ME2yMlc5QTZ7IN88US=> MorRV2FPT0WU
SNB75 M2POeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTJwOEi1N|Uh|ryP MXnTRW5ITVJ?
BFTC-905 NWLWXHUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnqT2VKSzVyPUKuPVAyQTFizszN NVzwW5FYW0GQR1XS
C-4-II M2L3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJwOUGzOVMh|ryP MnTCV2FPT0WU
MS-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXxTWVKSzVyPUKuPVY4PjlizszN M3rVWnNCVkeHUh?=
A375 MoLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknUTWM2OD1|LkC4NVg1KM7:TR?= MnjHV2FPT0WU
KYSE-70 MlvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPBcZh{UUN3ME2zMlA5QDh{IN88US=> NVToPZNpW0GQR1XS
KYSE-510 NFrNbGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGwd3JmUUN3ME2zMlExQTl3IN88US=> NHvrSYFUSU6JRWK=
LN-405 M3XXN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fYTmlEPTB;Mz6xN|UyQCEQvF2= NYf6U2g{W0GQR1XS
BOKU MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz0PVNjUUN3ME2zMlE1OjV4IN88US=> NEjOepJUSU6JRWK=
TE-10 MnTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmO0TWM2OD1|LkG3N|YzKM7:TR?= M3vEbnNCVkeHUh?=
MKN1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTNwMUi0PFMh|ryP NIPSXppUSU6JRWK=
M059J M3\6[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTNwMkCxO|Mh|ryP NUnBVoR3W0GQR1XS
GOTO MlfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jXdGlEPTB;Mz6yNlA{QSEQvF2= MmnFV2FPT0WU
DK-MG MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHUTWM2OD1|LkK1PVc3KM7:TR?= M4DQR3NCVkeHUh?=
NCI-H727 MmH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PFNWlEPTB;Mz6yOlU5KM7:TR?= NUmx[m13W0GQR1XS
NB12 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml71TWM2OD1|LkOzNlI1KM7:TR?= M2nJbnNCVkeHUh?=
DOK M3PjXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HaTWlEPTB;Mz6zOlE5PiEQvF2= NHzLc4VUSU6JRWK=
KYSE-410 NXe5TGFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTITWM2OD1|LkO2Nlg4KM7:TR?= NHj0fIpUSU6JRWK=
AM-38 NEDzfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDYXFBKSzVyPUOuN|gxPTFizszN NFeyVJFUSU6JRWK=
GR-ST MmL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVriTWFuUUN3ME2zMlQ2PzN{IN88US=> NVPnUopGW0GQR1XS
D-247MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\6NHdKSzVyPUOuOFgzPjNizszN MX;TRW5ITVJ?
TE-8 Ml7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\sUWlEPTB;Mz60PVM{OyEQvF2= NVzWV3M4W0GQR1XS
LS-411N M4XT[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHX3OXNKSzVyPUOuOFk3QTJizszN MnzKV2FPT0WU
SK-MES-1 NH;4[oZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7qNlRYUUN3ME2zMlU3PDN|IN88US=> NF;EW4ZUSU6JRWK=
SF295 M37QUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljVTWM2OD1|Lk[xOVUzKM7:TR?= MV7TRW5ITVJ?
SK-MEL-30 M{KwOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLmTWM2OD1|Lk[1PVIyKM7:TR?= NWK3NW8{W0GQR1XS
LB2241-RCC NXrkNHJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;aNFh4UUN3ME2zMlY3OjZizszN NVG1[Xd7W0GQR1XS
PC-14 NYP5cJU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ewVWlEPTB;Mz62OlQ{PyEQvF2= NUPi[IhqW0GQR1XS
EW-7 NX;FPGt1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37BRmlEPTB;Mz62O|Y6OyEQvF2= NInYZplUSU6JRWK=
NMC-G1 NVr0[2pPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlS0TWM2OD1|LkexPFM4KM7:TR?= M1HLenNCVkeHUh?=
TE-441-T M3O4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLVOoRKSzVyPUOuO|MxOjhizszN NUPHeFRYW0GQR1XS
NCI-H1618 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnW3TWM2OD1|LkixPFc2KM7:TR?= NU\FUnlKW0GQR1XS
PANC-03-27 NWXqRoFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPWTWM2OD1|LkixPVE3KM7:TR?= NHva[lBUSU6JRWK=
NCI-H2228 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H4RmlEPTB;Mz64N|EzPiEQvF2= NIPTZ5lUSU6JRWK=
CAPAN-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTNwOEewNFkh|ryP MUHTRW5ITVJ?
KLE MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjKcYZQUUN3ME2zMlkxPjdizszN MlTPV2FPT0WU
Becker MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrkdZNKSzVyPUOuPVI5PDlizszN NXvTb41vW0GQR1XS
SK-PN-DW M2G0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP6TWM2OD12LkC3PVc1KM7:TR?= Ml3ZV2FPT0WU
Hs-578-T Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv6fmFMUUN3ME20MlA5OzB4IN88US=> MWnTRW5ITVJ?
RS4-11 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHi0c|BKSzVyPUSuNVEzPTVizszN M2jMbXNCVkeHUh?=
D-502MG MlXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nFRWlEPTB;ND6xOlk6PyEQvF2= NWDNPVNkW0GQR1XS
GI-1 NFvWZnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnvWmFKSzVyPUSuNlgzQTlizszN MYjTRW5ITVJ?
NCI-H209 MnXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnaUJpKSzVyPUSuN|M4QCEQvF2= NITEPGJUSU6JRWK=
SK-OV-3 Ml24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnpUGJMUUN3ME20MlQ5OTR7IN88US=> M4POb3NCVkeHUh?=
LOUCY Mk\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\OOJNKSzVyPUSuOFg1OzJizszN MVTTRW5ITVJ?
NCI-H69 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rJ[2lEPTB;ND61NVc6OyEQvF2= NEPhPZRUSU6JRWK=
SCC-9 NWLTOWg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTRwNUOxO|Ih|ryP NXjxNZpUW0GQR1XS
NCI-H526 NFvRdIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTRwNUmyPVMh|ryP NIT0cVBUSU6JRWK=
NCI-H2170 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3vUlY5UUN3ME20MlY3PzdzIN88US=> MnTNV2FPT0WU
SR MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfQR5JkUUN3ME20MlcxODR6IN88US=> NWfENFdMW0GQR1XS
CMK NFL1T25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWThOHZKUUN3ME20MlczOTBzIN88US=> MkK0V2FPT0WU
COLO-829 M4rFR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVz0b2M1UUN3ME20Mlc4ODR|IN88US=> NV7xcnFsW0GQR1XS
HuO-3N1 M1zhUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGi4[2pKSzVyPUSuPFMzQDFizszN MlLYV2FPT0WU
5637 NWLZfVRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXqTWM2OD12LkmwOFg4KM7:TR?= NYD2XHRuW0GQR1XS
A253 MnX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\TcmlEPTB;ND65O|cxQCEQvF2= Mm\iV2FPT0WU
NB10 M4mwTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml[3TWM2OD13LkC3OFk4KM7:TR?= NFz5bY5USU6JRWK=
SF539 M1HjR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfqc5RvUUN3ME21MlA6QTV7IN88US=> NXz4RpN4W0GQR1XS
HAL-01 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\3SG9KSzVyPUWuNVQ3PDVizszN MX7TRW5ITVJ?
MHH-ES-1 NXHrS2F6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjh[|VKSzVyPUWuNVY6OjVizszN Ml\TV2FPT0WU
DEL NVWyO5NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr5TWM2OD13LkK3OVgzKM7:TR?= NYDQU29UW0GQR1XS
NCI-H1299 MmfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTVwM{WwNFch|ryP MnLzV2FPT0WU
ChaGo-K-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfrTWM2OD13LkO1NVA4KM7:TR?= M1n1OnNCVkeHUh?=
HMV-II Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjzTWM2OD13LkO5OFMh|ryP MnXUV2FPT0WU
NB69 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXkPW9mUUN3ME21MlM6PjNzIN88US=> MknOV2FPT0WU
NCI-H1882 M1nGOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vJZmlEPTB;NT60N|M3PCEQvF2= NFPmZW9USU6JRWK=
SNU-475 Mn;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoH3TWM2OD13LkS3NVcyKM7:TR?= M4r0W3NCVkeHUh?=
RXF393 MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnXTWM2OD13LkS4OFk1KM7:TR?= MVXTRW5ITVJ?
CAL-51 M1zNeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rEUGlEPTB;NT62Nlg2OyEQvF2= NGnMXWxUSU6JRWK=
SW1573 NIfDU5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTVwNkO1N|Qh|ryP MljVV2FPT0WU
GCT M4jCXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTVwN{W5Nlkh|ryP MYDTRW5ITVJ?
COR-L88 NXrHcZVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTYTWM2OD13Lke2PFQ3KM7:TR?= M3u1O3NCVkeHUh?=
MDA-MB-134-VI MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTVwOEe1N|Yh|ryP NXfQTXdkW0GQR1XS
NB5 NFvrclJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37ZfGlEPTB;NT65NlQ1KM7:TR?= MYTTRW5ITVJ?
GMS-10 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;TdHBKSzVyPUWuPVY5PjFizszN MlnZV2FPT0WU
CHP-212 NYDDc5VjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfUZVR{UUN3ME22MlQ5OjZ5IN88US=> MmnwV2FPT0WU
TE-11 M1j2[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYf5U|U4UUN3ME22MlU2OTh{IN88US=> M{\1UnNCVkeHUh?=
SW962 NXH0bow6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTZwNkW3O|Qh|ryP M1[w[3NCVkeHUh?=
MZ2-MEL NEiyOHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L4OGlEPTB;Nj64NlAyOSEQvF2= M3LZXXNCVkeHUh?=
C-33-A NG\tV5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37uW2lEPTB;Nj65NVY5QCEQvF2= MV3TRW5ITVJ?
IGR-1 MkTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojITWM2OD14Lkm3PFI3KM7:TR?= NF\Vbm1USU6JRWK=
MOLT-4 M4T2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTdwMUW0NFYh|ryP NFX6N4tUSU6JRWK=
NCI-H1650 NV7RUJBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rmbGlEPTB;Nz6yO|A1PiEQvF2= MYPTRW5ITVJ?
AsPC-1 NEXoWpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknLTWM2OD15LkK4OlA2KM7:TR?= MVvTRW5ITVJ?
SNU-C2B NX[yUGo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnTTWM2OD15LkK5OVcyKM7:TR?= NHjCZVdUSU6JRWK=
MKN7 NEXD[WtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HTfGlEPTB;Nz6zO|I{PSEQvF2= NYj6WGpXW0GQR1XS
SW620 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rOXGlEPTB;Nz6zPFIxPSEQvF2= NHLCemFUSU6JRWK=
SK-MEL-28 NGnaPXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXLV25kUUN3ME23MlQxPzl6IN88US=> NInVOHNUSU6JRWK=
TE-6 NX;XUHJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfic|BTUUN3ME23MlQ1QTB6IN88US=> NW\5W2x6W0GQR1XS
D-263MG MkTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3vSW1OUUN3ME23MlQ2PzZ{IN88US=> M1H2dnNCVkeHUh?=
NCI-H1355 M2DES2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LuUWlEPTB;Nz63O|AzQSEQvF2= M2[4XHNCVkeHUh?=
DSH1 M{e3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTdwN{m3OlIh|ryP MYDTRW5ITVJ?
NCI-H460 NV33XlNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDZOFNKSzVyPUiuNFA3QTRizszN MXvTRW5ITVJ?
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GCIY NWf6VFA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJ3LkK4O|ch|ryP MnHUV2FPT0WU
NUGC-3 NUjnU3JnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\HTWM2OD1{NT6zN|E3KM7:TR?= NVryUIU3W0GQR1XS
LNCaP-Clone-FGC NH7oc5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\DVGlEPTB;MkWuN|Q6QCEQvF2= NWPESJRrW0GQR1XS
PA-1 NHyzUlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\D[nJKSzVyPUK1MlY5OzNizszN NWXNc3liW0GQR1XS
OE33 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrWTHJKSzVyPUK1MlY5PTNizszN NGftcmhUSU6JRWK=
HT-29 MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPWXIxKSzVyPUK1Mlc5PzlizszN NG\mfWlUSU6JRWK=
RCM-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfZeIlKSzVyPUK1Mlk3PTZizszN NEHHO5RUSU6JRWK=
NCI-H1522 Ml7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHhV5JYUUN3ME2yOU46QTFzIN88US=> M2TmV3NCVkeHUh?=
LB373-MEL-D NH;XSnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXDTWM2OD1{Nj6xO|A5KM7:TR?= M1j3bXNCVkeHUh?=
NCI-H1436 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDkTWM2OD1{Nj6yO|M5KM7:TR?= MYLTRW5ITVJ?
COLO-824 NUXoRXhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJ4LkSwNFIh|ryP NH3BPItUSU6JRWK=
CP50-MEL-B MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfOVHhKSzVyPUK2MlU3PzVizszN NH3zPJVUSU6JRWK=
EGI-1 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJ5LkK2PVgh|ryP MkXsV2FPT0WU
LAN-6 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFz1N3hKSzVyPUK3MlM2QThizszN MXvTRW5ITVJ?
GAK NVzqXphlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJ5LkSyNlUh|ryP MmT0V2FPT0WU
MDA-MB-175-VII MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PrWWlEPTB;MkeuOVA2OyEQvF2= NIexb4VUSU6JRWK=
JVM-2 NWTjOlQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTJ5Lk[2NlIh|ryP MmD6V2FPT0WU
UACC-257 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJ5Lk[4O|gh|ryP NYTIW5dtW0GQR1XS
SW1783 Ml31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTRPYVKSzVyPUK3Mlc4QDNizszN MoDQV2FPT0WU
HT-3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTJ6LkKxOlYh|ryP NFHvT2ZUSU6JRWK=
RL MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHpV5FKSzVyPUK4MlU6OTFizszN M1rkd3NCVkeHUh?=
TK10 NVWwN4VMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUG2cXVwUUN3ME2yPE43PTN3IN88US=> MULTRW5ITVJ?
HT55 NWTNcpdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PjO2lEPTB;MkmuNFU3PSEQvF2= NEfKR5RUSU6JRWK=
BT-20 NY[3eotsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISy[IRKSzVyPUK5MlA2QDZizszN MUjTRW5ITVJ?
TGBC24TKB NEPPO49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXpSZg{UUN3ME2yPU4yQDNzIN88US=> NVfie2d3W0GQR1XS
HSC-2 M{e3b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXZRolOUUN3ME2yPU4{ODBzIN88US=> MVLTRW5ITVJ?
COLO-205 MnK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfYTWM2OD1{OT6zPVQ1KM7:TR?= M3zrVHNCVkeHUh?=
GT3TKB NVjVXGxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH2xTlZKSzVyPUK5MlY5PzdizszN M1j4VXNCVkeHUh?=
T47D NInFRpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nrfmlEPTB;MkmuPFU5OiEQvF2= MV;TRW5ITVJ?
OMC-1 M2rBfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEmz[|RKSzVyPUOwMlE6OTlizszN MkLqV2FPT0WU
PFSK-1 NWC3UWRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDhTWM2OD1|MT6yOlU6KM7:TR?= NV:3V5JLW0GQR1XS
JEG-3 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrYSFBKSzVyPUOxMlM2PjFizszN MnXzV2FPT0WU
RD MnXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\2XmlEPTB;M{GuOVEyPSEQvF2= MmO1V2FPT0WU
NCI-H64 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfkenJEUUN3ME2zNk41OTd7IN88US=> M1rNSHNCVkeHUh?=
DMS-114 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWj2UllyUUN3ME2zNk41OTh{IN88US=> M{[xdXNCVkeHUh?=
NCI-H661 M{PDeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD4bWNkUUN3ME2zNk43PTBzIN88US=> NIj5XIhUSU6JRWK=
CAL-148 NV;LeZdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTN{Lk[2OlUh|ryP M1\HNXNCVkeHUh?=
HuP-T3 M{Xve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTN{LkmzN|gh|ryP NGHSRXBUSU6JRWK=
ES4 M3HlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrCZYFKSzVyPUOzMlE4ODVizszN NELtdXVUSU6JRWK=
Ca9-22 M{fxVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\r[mlEPTB;M{OuOFYxOSEQvF2= M1v0Z3NCVkeHUh?=
LP-1 NEC2fnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWX6VoV3UUN3ME2zOE4xQSEQvF2= MoTSV2FPT0WU
AU565 M3ToXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPN[JRKSzVyPUO0MlUxPjlizszN M33kR3NCVkeHUh?=
MDA-MB-453 M{HuTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHRe|RKSzVyPUO1MlE1OjZizszN M1Xkd3NCVkeHUh?=
SNU-C1 NVr2bGZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPHPGRvUUN3ME2zOU4yPzFizszN M3nwXHNCVkeHUh?=
SW13 NG\vW2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7ZTWM2OD1|NT60NFc3KM7:TR?= MVXTRW5ITVJ?
NCI-H2122 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTN3LkW1PVgh|ryP M{P6d3NCVkeHUh?=
NCI-H1395 MoTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTidWxxUUN3ME2zOU43PjlzIN88US=> MVXTRW5ITVJ?
J-RT3-T3-5 NFjXRXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfETWM2OD1|Nj6wNlk1KM7:TR?= MnPzV2FPT0WU
COR-L279 NGDZUnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi5TWM2OD1|Nj6xPVgyKM7:TR?= MXnTRW5ITVJ?
ATN-1 NHHRTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmS5TWM2OD1|Nj64OVE3KM7:TR?= NXnHN3JmW0GQR1XS
HCC2998 NV7KPJlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3MNW9ZUUN3ME2zOk45PTdzIN88US=> NFLJV4hUSU6JRWK=
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DV-90 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPzb3hUUUN3ME2zOk46ODZ5IN88US=> MofvV2FPT0WU
ES8 MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXyellJUUN3ME2zOk46OzF6IN88US=> MnnqV2FPT0WU
YAPC MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\OWmIzUUN3ME2zOk46PjV2IN88US=> NEK0RY5USU6JRWK=
HCC1599 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLhcJRKSzVyPUO3MlE3OThizszN Moq1V2FPT0WU
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THP-1 M134VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\VUWNKSzVyPUO3MlI5PjhizszN NInYRZFUSU6JRWK=
OCUB-M MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXT[FJoUUN3ME2zO{4zQDlzIN88US=> NX\CO296W0GQR1XS
NCI-H1693 NF;WNlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPuTWM2OD1|Nz6zNlM{KM7:TR?= NEfnZmRUSU6JRWK=
NCI-H345 NEPx[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3PXWV[UUN3ME2zO{4{PjJ2IN88US=> NGDIbWJUSU6JRWK=
COLO-800 M1KyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\2eolKSzVyPUO3MlU3PyEQvF2= MXfTRW5ITVJ?
COLO-320-HSR MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3QZpNKSzVyPUO4MlM1QTJizszN MmHEV2FPT0WU
NCI-H596 NWOxfms6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jzO2lEPTB;M{iuOFQ5QSEQvF2= NGP6N3lUSU6JRWK=
NCI-H187 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTN6LkezOFQh|ryP NUn6O3R5W0GQR1XS
ECC4 NHfYZoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojrTWM2OD1|OT6wPFE1KM7:TR?= NIDU[|RUSU6JRWK=
KP-4 NWLSOFZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGS2NmJKSzVyPUO5MlEzOzVizszN NXfzOJBCW0GQR1XS
NCI-H2227 NYrkZXhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHnWZVwUUN3ME2zPU4{QTR7IN88US=> MmLmV2FPT0WU
22RV1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfMTWM2OD1|OT64N|k5KM7:TR?= Mk[1V2FPT0WU
SAS NGTSepBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTRyLkC5OkDPxE1? MVLTRW5ITVJ?
PANC-10-05 M{j6UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTRyLkG4Nlgh|ryP M376eHNCVkeHUh?=
MDA-MB-468 NWCwdXdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTRyLkWzOFYh|ryP M2PVZnNCVkeHUh?=
RPMI-7951 NVTPOGlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTRzLkKwO|Uh|ryP MonTV2FPT0WU
BB49-HNC NUjzSVdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHkTWM2OD12MT6yNVc6KM7:TR?= Mn2xV2FPT0WU
23132-87 Mn63S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknoTWM2OD12MT6yO|MzKM7:TR?= NUD4UWx6W0GQR1XS
HCC1569 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmS5TWM2OD12MT6yPFg2KM7:TR?= NF3YOHBUSU6JRWK=
CP66-MEL MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHSVYZKSzVyPUSyMlE5QDZizszN MWTTRW5ITVJ?
K-562 Mmn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;oUow5UUN3ME20Nk4zQDV2IN88US=> NH3rbVJUSU6JRWK=
OCI-AML2 NFOx[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXpTWM2OD12Mj64PVc1KM7:TR?= MnTQV2FPT0WU
SW756 NFLxS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH3PJc1UUN3ME20N{4xOzh6IN88US=> M3TMSHNCVkeHUh?=
M14 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTR|LkOxPFkh|ryP Ml60V2FPT0WU
NCI-H1623 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTR|LkS2OEDPxE1? NFqzemFUSU6JRWK=
KNS-81-FD MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWwVHhKSzVyPUSzMlc3OiEQvF2= NFnyOZNUSU6JRWK=
TGBC1TKB NILqOWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\OTWM2OD12Mz65NFk6KM7:TR?= NHP2[oZUSU6JRWK=
RERF-LC-MS MlPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTHTWM2OD12Mz65NlgyKM7:TR?= NEfRbndUSU6JRWK=
PC-3 M2nQZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXGdoNKSzVyPUS0MlQ{PDdizszN Mn\KV2FPT0WU
HuP-T4 MmXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[1TWM2OD12ND60OFc1KM7:TR?= NVr2Xm15W0GQR1XS
NCI-H510A MnvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TWfGlEPTB;NESuO|A5KM7:TR?= NHLCOGdUSU6JRWK=
LB2518-MEL M2XzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFL0fWlKSzVyPUS0Mlc6OzdizszN Mne3V2FPT0WU
TE-5 MlK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\6TWM2OD12NT65OVgyKM7:TR?= NYD5dY1lW0GQR1XS
EW-24 NWC0XHZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTR4LkG3NlMh|ryP M2mxR3NCVkeHUh?=
LB647-SCLC NGfrXXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfkWGxKSzVyPUS2MlIyPTVizszN NEnZU41USU6JRWK=
NCI-H524 MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVqxVFJNUUN3ME20Ok44OTh3IN88US=> NU\0TnlFW0GQR1XS
EW-11 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTCTWM2OD12Nj65N|c{KM7:TR?= MmPMV2FPT0WU
KALS-1 M4D1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKwTWM2OD12Nz6yNFY3KM7:TR?= MXLTRW5ITVJ?
BT-474 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEC3cpdKSzVyPUS3MlQzOTZizszN MmHiV2FPT0WU
SK-N-AS M1y3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTR5Lki4PEDPxE1? NUDMNI1yW0GQR1XS
HCC2157 NIDkc2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTKTWM2OD12OD6wO|Yh|ryP MnTFV2FPT0WU
HCC1954 NEjsdm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzUbG5vUUN3ME20PE4yPzB2IN88US=> M2rC[3NCVkeHUh?=
FADU NWrWcnE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTR6LkOwN|Eh|ryP Mnf0V2FPT0WU
S-117 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jUN2lEPTB;NEiuN|gyPSEQvF2= MX;TRW5ITVJ?
LS-1034 MmX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HPcmlEPTB;NEiuO|A3PyEQvF2= NVPOcnRXW0GQR1XS
CAMA-1 NFvrZ5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTR7LkW1OFMh|ryP MkHqV2FPT0WU
LU-134-A NIHpTnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\DeHFKSzVyPUS5MlgxQDVizszN NIjwdJhUSU6JRWK=
NCI-H1838 NUPBNXh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTR7LkiwPFch|ryP MV\TRW5ITVJ?

... 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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