Ponatinib (AP24534) 化学構造
分子量: 532.56

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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 MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\2RWlEPTB;MD6wNFAxODByM{W5JO69VQ>? MYLTRW5ITVJ?
MV-4-11 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7PTWM2OD1yLkCwNFA6PTZizszN M{fWTHNCVkeHUh?=
MEG-01 NEPqbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;mS4NtUUN3ME2wMlAxODF{ODFOwG0> NE\QTFJUSU6JRWK=
LAMA-84 NH63PJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfDVWVKSzVyPUCuNFAxOTZ3IN88US=> NHj2c2VUSU6JRWK=
CGTH-W-1 M1jyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLTOlBKSzVyPUCuNFAyPjlizszN M1S0[nNCVkeHUh?=
KASUMI-1 NHTaRYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Pp[2lEPTB;MD6wNFIyPyEQvF2= MmWwV2FPT0WU
BE-13 M{fTWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLxTWM2OD1yLkCwNlU6KM7:TR?= NWH2PHNEW0GQR1XS
CTV-1 M4KzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwMEC1NlEh|ryP M4Pt[3NCVkeHUh?=
NKM-1 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XXU2lEPTB;MD6wNFY2PSEQvF2= NIXVNnJUSU6JRWK=
MONO-MAC-6 NXf4NZE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrPU4FKSzVyPUCuNFA5OzdizszN NVruc|VMW0GQR1XS
A204 NGf2cJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu2eYdTUUN3ME2wMlAyOjF6IN88US=> M33SbHNCVkeHUh?=
GDM-1 NFzFR4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfHTWM2OD1yLkCxPFM{KM7:TR?= M4\IUXNCVkeHUh?=
AN3-CA MlzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHMTWM2OD1yLkCxPFc{KM7:TR?= MnHRV2FPT0WU
BL-70 MnjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TZc2lEPTB;MD6wNlE6QSEQvF2= NHzCbVJUSU6JRWK=
Daudi MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwMEK1N|ch|ryP M{Xv[3NCVkeHUh?=
KU812 NVXFZohQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXNc|hKSzVyPUCuNFI5PDhizszN MVLTRW5ITVJ?
KG-1 M{frT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\2S4lKSzVyPUCuNFMzQTRizszN NGj2WJRUSU6JRWK=
DOHH-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13HdGlEPTB;MD6wOFgxOyEQvF2= NHPufGdUSU6JRWK=
HuO9 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWyTWM2OD1yLkC1OFQ5KM7:TR?= Mlr1V2FPT0WU
EB2 M3qxdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK1TWM2OD1yLkC1OVc3KM7:TR?= NFPKXohUSU6JRWK=
G-402 Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4mxNWlEPTB;MD6wOlM1OSEQvF2= NGTv[YxUSU6JRWK=
SU-DHL-1 MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTBwME[zO|kh|ryP NFzudFlUSU6JRWK=
NCI-H719 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36wXWlEPTB;MD6wO|g5QCEQvF2= NEHOfmtUSU6JRWK=
MLMA NVXhT4ZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nlUWlEPTB;MD6wPVA3KM7:TR?= NGTjXINUSU6JRWK=
KM12 M{KzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HrRmlEPTB;MD6wPVc{PyEQvF2= NGfsNXVUSU6JRWK=
SUP-T1 NGPBPIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfnbJJLUUN3ME2wMlA6QTh{IN88US=> NGXYb3pUSU6JRWK=
MZ1-PC MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17Q[2lEPTB;MD6xNVM{PiEQvF2= NX3zfXZPW0GQR1XS
MFE-296 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH4NJRiUUN3ME2wMlEyQDN7IN88US=> NGfneJBUSU6JRWK=
ALL-PO NYq4VpkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonXTWM2OD1yLkGyOFQ{KM7:TR?= MYDTRW5ITVJ?
GB-1 NUOzWGRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17Ke2lEPTB;MD6xNlUyOiEQvF2= M2HJWXNCVkeHUh?=
SIG-M5 M{fMbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTSTWM2OD1yLkGzN|ch|ryP NXXySZdpW0GQR1XS
P30-OHK NFG3W2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTBwMUW2O|Ih|ryP M2H5Z3NCVkeHUh?=
NCI-H716 NXHvZnZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwMU[yOlYh|ryP NIfNW4VUSU6JRWK=
MPP-89 NF3VR5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTBwMU[5N|Mh|ryP NEXHbHNUSU6JRWK=
SF126 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\kUG51UUN3ME2wMlE4ODZ|IN88US=> M3\5WnNCVkeHUh?=
CTB-1 MmC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFK1PVFKSzVyPUCuNVc{OTZizszN NGD0ZlNUSU6JRWK=
CA46 NELSV|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHNbpNKSzVyPUCuNVc1QDlizszN M4\xTnNCVkeHUh?=
NCI-H520 NEW3Z21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfmdZhKSzVyPUCuNVc4OzJizszN NHXwfmxUSU6JRWK=
CAL-85-1 NEL0bpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXzTWM2OD1yLkG3PVI4KM7:TR?= NH;nXJJUSU6JRWK=
NCI-H2342 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2ThXWlEPTB;MD6xPFU4PyEQvF2= MoruV2FPT0WU
697 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3roVWlEPTB;MD6xPFg4OSEQvF2= NYOwO5ZKW0GQR1XS
NY NYXYVlBST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\pSYVHUUN3ME2wMlE6Ojh5IN88US=> M4rhWnNCVkeHUh?=
T98G MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fqWWlEPTB;MD6xPVMyQCEQvF2= NFHhOmpUSU6JRWK=
NCI-H1703 NGfhS5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjKdGtKSzVyPUCuNVk3OTVizszN M2fLTXNCVkeHUh?=
NCI-H2087 NUnlPZdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf2PYM5UUN3ME2wMlIxPDN7IN88US=> M17sNnNCVkeHUh?=
PF-382 NWi0O41FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvzXIEyUUN3ME2wMlIxQDd|IN88US=> M4rKSXNCVkeHUh?=
HCT-116 M1vSWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS3TWM2OD1yLkKxNFY6KM7:TR?= Mm\pV2FPT0WU
CAKI-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofsTWM2OD1yLkKxOlY3KM7:TR?= Mm\kV2FPT0WU
CCF-STTG1 NVnSPG5WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLxOWZtUUN3ME2wMlIzPDd3IN88US=> MXvTRW5ITVJ?
D-392MG MnTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVric|JZUUN3ME2wMlI{OTd5IN88US=> NYrUSpk2W0GQR1XS
RT-112 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwMkO3PVUh|ryP M3HHSnNCVkeHUh?=
MES-SA NXLPOnJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLXTWM2OD1yLkK0NVg4KM7:TR?= MXnTRW5ITVJ?
LC-2-ad NWDUSWtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFr0PW1KSzVyPUCuNlQzPjVizszN Mke2V2FPT0WU
NOS-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[1TWM2OD1yLkK0N|Y4KM7:TR?= NUPTUGNVW0GQR1XS
NALM-6 M4SzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVq4XnhSUUN3ME2wMlI2PTR|IN88US=> NV:3fXN4W0GQR1XS
TE-15 M1fsfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{iw[mlEPTB;MD6yOlA6OSEQvF2= M4S5WnNCVkeHUh?=
786-0 NYHHPIdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPo[FlKSzVyPUCuNlYzOjhizszN M4TWdHNCVkeHUh?=
IST-MES1 NFnpUW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXle|hsUUN3ME2wMlI3QDJ7IN88US=> M3yzbHNCVkeHUh?=
KYSE-180 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGn1RY5KSzVyPUCuNlY5QTFizszN MlHDV2FPT0WU
YT MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFu3W2lKSzVyPUCuNlY6PzRizszN MYHTRW5ITVJ?
A427 NFyyN5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmL0TWM2OD1yLkK3NlY1KM7:TR?= NF7RUIdUSU6JRWK=
KYSE-450 NYi5NmNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jYNGlEPTB;MD6yO|MzQSEQvF2= NIjtZ2ZUSU6JRWK=
HuH-7 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHQTWM2OD1yLkK3O|Y{KM7:TR?= M1LHVXNCVkeHUh?=
CAS-1 NXLrRpNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTBwMkizNFMh|ryP MYnTRW5ITVJ?
KURAMOCHI NYTU[|BET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGj2NpNKSzVyPUCuNlg1OTlizszN NXG4UZJPW0GQR1XS
ACHN Ml7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIeyb4dKSzVyPUCuNlk{OjNizszN NF7ObXVUSU6JRWK=
HGC-27 NHmzXJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TNd2lEPTB;MD6yPVM2OyEQvF2= NIfjO3NUSU6JRWK=
A172 NUPBfIdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnmb5RKSzVyPUCuNlk2PzdizszN MnX2V2FPT0WU
SNU-449 Mkn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwMkm5OlQh|ryP MYnTRW5ITVJ?
SW982 NV;lT2ZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7HRo5qUUN3ME2wMlI6QTd6IN88US=> MWrTRW5ITVJ?
EFO-21 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj6So5KSzVyPUCuN|A1OTFizszN Mnu4V2FPT0WU
NCI-H2030 M1T6VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vKTWlEPTB;MD6zNVE3PCEQvF2= NGnET|lUSU6JRWK=
HT-144 MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPjW3lKSzVyPUCuN|EzQCEQvF2= NXzKZ4VIW0GQR1XS
MFE-280 Mn3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyyU3dnUUN3ME2wMlMyPDV|IN88US=> MnjMV2FPT0WU
SK-LU-1 NFvVcYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vVXGlEPTB;MD6zNVQ3PiEQvF2= NV\v[|dNW0GQR1XS
NCI-H2052 MkPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzvTWM2OD1yLkOxOFg1KM7:TR?= NVXZNGtMW0GQR1XS
SK-HEP-1 M{Dx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17wNGlEPTB;MD6zN|M3QCEQvF2= NEHIWFZUSU6JRWK=
QIMR-WIL NE\2UZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL5VldCUUN3ME2wMlM{PDJ2IN88US=> MXLTRW5ITVJ?
A2780 NIPmT|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwM{SzNFQh|ryP NIDDVYxUSU6JRWK=
ACN MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jVN2lEPTB;MD6zOFg4OyEQvF2= M4nIeXNCVkeHUh?=
BxPC-3 NV;RRpBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvL[G5YUUN3ME2wMlM1QTh7IN88US=> MlH2V2FPT0WU
BCPAP NYfEVXdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHSTHhkUUN3ME2wMlM3ODBzIN88US=> MYPTRW5ITVJ?
HOP-62 NETJOGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwM{[xNFYh|ryP NF[zO41USU6JRWK=
SW1710 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEC1NJZKSzVyPUCuN|Y1PTVizszN NV:5VHYyW0GQR1XS
OPM-2 M4\SeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojjTWM2OD1yLkO2OFc{KM7:TR?= NIi3UWhUSU6JRWK=
DBTRG-05MG MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTBwM{iwOVQh|ryP MYrTRW5ITVJ?
SK-MEL-24 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvqRml5UUN3ME2wMlM6PzlzIN88US=> MVfTRW5ITVJ?
8305C MnfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwM{m3PVMh|ryP M1jybnNCVkeHUh?=
OVCAR-4 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTBwNEG1PFYh|ryP M4[2XnNCVkeHUh?=
HLE MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jE[GlEPTB;MD60NVg3KM7:TR?= MYnTRW5ITVJ?
NCI-H747 NHjLenJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7CSJFDUUN3ME2wMlQzOTN5IN88US=> MVvTRW5ITVJ?
SW780 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILkeWZKSzVyPUCuOFI{PDZizszN MYXTRW5ITVJ?
KYSE-150 NVX1fYVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjJ[GdFUUN3ME2wMlQzPDF3IN88US=> M3W4cnNCVkeHUh?=
H4 NHyyZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwNEK0OVEh|ryP NIfJS2JUSU6JRWK=
SW1088 NVnvfGZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjK[o1{UUN3ME2wMlQ1OzlizszN NFK5O25USU6JRWK=
SF268 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojjTWM2OD1yLkS0PFYh|ryP MW\TRW5ITVJ?
RT4 Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLJfHdKSzVyPUCuOFUyOTFizszN NIHnfoNUSU6JRWK=
NCI-H522 MlrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe0TWM2OD1yLkS1Nlch|ryP Mn3DV2FPT0WU
LCLC-97TM1 NHjvR4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTOfWFEUUN3ME2wMlQ3OTl3IN88US=> M1XDbHNCVkeHUh?=
CAL-39 M2TUeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfNXpdKSzVyPUCuOFY2OTlizszN MmrMV2FPT0WU
CAL-120 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTBwNEe2OFMh|ryP MVTTRW5ITVJ?
ESS-1 Mn3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O2VGlEPTB;MD60O|gzOSEQvF2= NEOwWJRUSU6JRWK=
KARPAS-45 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwNEi5N|Mh|ryP Ml\vV2FPT0WU
DU-4475 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;2XpRoUUN3ME2wMlQ6PTFzIN88US=> M4n5XXNCVkeHUh?=
VMRC-RCZ NFHzdIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfpTWM2OD1yLkS5PVA1KM7:TR?= M1jDZnNCVkeHUh?=
HOS NETQRoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvaTWM2OD1yLkWwN|Y2KM7:TR?= NHLiPFFUSU6JRWK=
MOLT-16 M{m1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoqxTWM2OD1yLkWxPFA5KM7:TR?= MVfTRW5ITVJ?
RPMI-6666 M4HFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwNUKxN|Uh|ryP M1TiU3NCVkeHUh?=
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EHEB MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\YWJZKSzVyPUCuOVIyQDJizszN MWHTRW5ITVJ?
MFH-ino M1rKcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnMTWM2OD1yLkWyN|UyKM7:TR?= NF7pNYVUSU6JRWK=
A4-Fuk NF\KNJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13adGlEPTB;MD61NlUzQCEQvF2= M1faNnNCVkeHUh?=
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MC-IXC NV7qSm14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzUbnRMUUN3ME2yMlAzOjd|IN88US=> NFrk[XZUSU6JRWK=
COLO-678 NXvQO3FCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGW3SVVKSzVyPUKuNFQzODdizszN M2e3NXNCVkeHUh?=
MEL-JUSO MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTJwMEe4OVEh|ryP MUjTRW5ITVJ?
HCC38 MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nWfmlEPTB;Mj6wPFQ{OyEQvF2= MXnTRW5ITVJ?
UACC-62 M2TJR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoW4TWM2OD1{LkC4PFU2KM7:TR?= MmTyV2FPT0WU
OAW-42 M2Pjemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlP6TWM2OD1{LkC5O|EyKM7:TR?= NUO4bo81W0GQR1XS
LB996-RCC NGjYUJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJwMUO4NVch|ryP MWTTRW5ITVJ?
COR-L105 NGL6dVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jS[GlEPTB;Mj6xOlM4OyEQvF2= NIjQSVRUSU6JRWK=
RCC10RGB M4jEOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPUTWM2OD1{LkG4OVc3KM7:TR?= NVPLe|dCW0GQR1XS
A431 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj5TWM2OD1{LkG5NFE6KM7:TR?= NGnvXYZUSU6JRWK=
NCI-H292 NVmydHFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7XU5V1UUN3ME2yMlI{QTVzIN88US=> MmHzV2FPT0WU
SK-UT-1 NFLtTWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDqUYxyUUN3ME2yMlM{OTh2IN88US=> M1LhUXNCVkeHUh?=
PANC-08-13 NWX3R25tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJwM{OyN|Uh|ryP MUTTRW5ITVJ?
ST486 NV7nVlhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HxdWlEPTB;Mj60NVA1QCEQvF2= M2rjenNCVkeHUh?=
SJSA-1 NFrxTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3HRpZKSzVyPUKuOFEzPzFizszN NVXMZYl6W0GQR1XS
RKO M2LQZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O4UWlEPTB;Mj60NlAzQSEQvF2= M3fGeHNCVkeHUh?=
NCI-H1793 MojnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfDb2J6UUN3ME2yMlQ1ODJ7IN88US=> NHPofmJUSU6JRWK=
639-V MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P2RWlEPTB;Mj60OVM5OiEQvF2= NV2xUXVlW0GQR1XS
ES3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjhOopKSzVyPUKuOFk4OzdizszN NI\qeHlUSU6JRWK=
NCI-H1792 NYm2PWRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q1[WlEPTB;Mj61OlgzPiEQvF2= M{m3OXNCVkeHUh?=
NCI-H1651 MnT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXXbm5tUUN3ME2yMlU5OjFizszN M4jwO3NCVkeHUh?=
SN12C MnzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHSTWM2OD1{LkW4OFg4KM7:TR?= NGDUNVFUSU6JRWK=
COLO-679 M33tXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXzOWdRUUN3ME2yMlU5PjB3IN88US=> Mo\kV2FPT0WU
U-118-MG M{jFbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fRVmlEPTB;Mj61PFg4OiEQvF2= M{jqSnNCVkeHUh?=
Ramos-2G6-4C10 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTSOI9wUUN3ME2yMlY1QDB5IN88US=> MX;TRW5ITVJ?
HCT-15 Ml;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnxdFZKSzVyPUKuOlg4QTJizszN MXTTRW5ITVJ?
MDA-MB-157 NETSXoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Ppc2lEPTB;Mj63NFc1PyEQvF2= Mnv2V2FPT0WU
K5 NXPFXWlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLzSXYzUUN3ME2yMlcyQDR3IN88US=> MXXTRW5ITVJ?
MKN45 NEDpXZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfSTWM2OD1{LkezN|Y3KM7:TR?= NWfUS2xlW0GQR1XS
DMS-273 M2[wN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTJwN{W2N|Ih|ryP MU\TRW5ITVJ?
C8166 NVn1R2VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLaU2hqUUN3ME2yMlc5PTF|IN88US=> M1PBcXNCVkeHUh?=
Calu-3 M1\YNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:5[mlEPTB;Mj63PFk3QSEQvF2= NIfKc|BUSU6JRWK=
SNB75 Mn3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfib|EyUUN3ME2yMlg5PTN3IN88US=> NWTHNpYyW0GQR1XS
BFTC-905 MnXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTJwOUCxPVEh|ryP MkWwV2FPT0WU
C-4-II MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjWSpdpUUN3ME2yMlkyOzV|IN88US=> MnmyV2FPT0WU
MS-1 NVLiN|ZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoK5TWM2OD1{Lkm2O|Y6KM7:TR?= NHX0VZNUSU6JRWK=
A375 NITQdGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTZUYpnUUN3ME2zMlA5OTh2IN88US=> NGGxXpVUSU6JRWK=
KYSE-70 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoO2TWM2OD1|LkC4PFgzKM7:TR?= Mme4V2FPT0WU
KYSE-510 M4\nRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUT3PWVJUUN3ME2zMlExQTl3IN88US=> Mn;DV2FPT0WU
LN-405 MorkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3niS2lEPTB;Mz6xN|UyQCEQvF2= NFnDOFhUSU6JRWK=
BOKU NFT1XnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:3d|JKUUN3ME2zMlE1OjV4IN88US=> M2ruT3NCVkeHUh?=
TE-10 NXnZZmtqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTNwMUezOlIh|ryP MU\TRW5ITVJ?
MKN1 NULFXJB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXhd3hKSzVyPUOuNVg1QDNizszN NV\JPW17W0GQR1XS
M059J M1;VfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGxVnRTUUN3ME2zMlIxOTd|IN88US=> M1jacnNCVkeHUh?=
GOTO MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTNwMkKwN|kh|ryP NYnnSGZsW0GQR1XS
DK-MG NIPyNpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTNwMkW5O|Yh|ryP NVv1WlRzW0GQR1XS
NCI-H727 NVXDd49WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnBe|U1UUN3ME2zMlI3PThizszN MknxV2FPT0WU
NB12 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnpNmRoUUN3ME2zMlM{OjJ2IN88US=> MV;TRW5ITVJ?
DOK NIT1XFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXG[nNRUUN3ME2zMlM3OTh4IN88US=> M1rSVHNCVkeHUh?=
KYSE-410 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPlTINbUUN3ME2zMlM3Ojh5IN88US=> MnnoV2FPT0WU
AM-38 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTlTWM2OD1|LkO4NFUyKM7:TR?= MnnBV2FPT0WU
GR-ST NXPWPVZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLKXGNvUUN3ME2zMlQ2PzN{IN88US=> NHfPb49USU6JRWK=
D-247MG MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPOT2pKSzVyPUOuOFgzPjNizszN M1fYfHNCVkeHUh?=
TE-8 M4jFRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTNwNEmzN|Mh|ryP MYnTRW5ITVJ?
LS-411N MnS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{j5d2lEPTB;Mz60PVY6OiEQvF2= M3X6fXNCVkeHUh?=
SK-MES-1 Mnv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rmd2lEPTB;Mz61OlQ{OyEQvF2= NX3BSGhKW0GQR1XS
SF295 NIjFXoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjNPY5KSzVyPUOuOlE2PTJizszN MX7TRW5ITVJ?
SK-MEL-30 NYK3PZNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7mc3FKSzVyPUOuOlU6OjFizszN Ml\KV2FPT0WU
LB2241-RCC MmexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrNNnBKSzVyPUOuOlYzPiEQvF2= MWLTRW5ITVJ?
PC-14 M1r6eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYKxdWJWUUN3ME2zMlY3PDN5IN88US=> NILuZ4dUSU6JRWK=
EW-7 MnrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTNwNke2PVMh|ryP NXntfXZXW0GQR1XS
NMC-G1 NFvIVG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTNwN{G4N|ch|ryP NWTLWZp4W0GQR1XS
TE-441-T MlrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTNwN{OwNlgh|ryP M1T1[nNCVkeHUh?=
NCI-H1618 MlzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTNwOEG4O|Uh|ryP M1qyS3NCVkeHUh?=
PANC-03-27 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXrc|BGUUN3ME2zMlgyQTF4IN88US=> MX3TRW5ITVJ?
NCI-H2228 NIe1ZWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjITWM2OD1|LkizNVI3KM7:TR?= MmT6V2FPT0WU
CAPAN-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PXb2lEPTB;Mz64O|AxQSEQvF2= M4PPbXNCVkeHUh?=
KLE NFzPTVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLRU4lKSzVyPUOuPVA3PyEQvF2= M2PIfXNCVkeHUh?=
Becker M{TLW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoP0TWM2OD1|LkmyPFQ6KM7:TR?= MUDTRW5ITVJ?
SK-PN-DW M1fpOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTRwMEe5O|Qh|ryP MW\TRW5ITVJ?
Hs-578-T MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjOTWM2OD12LkC4N|A3KM7:TR?= M1X3O3NCVkeHUh?=
RS4-11 NIrEbpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\TcYlKSzVyPUSuNVEzPTVizszN NXnaNG5iW0GQR1XS
D-502MG M3i4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTRwMU[5PVch|ryP MW\TRW5ITVJ?
GI-1 MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7rc5FoUUN3ME20MlI5Ojl7IN88US=> NYPFWFk4W0GQR1XS
NCI-H209 NVrZN3N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWGz[GZ7UUN3ME20MlM{PzhizszN MWDTRW5ITVJ?
SK-OV-3 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnntTWM2OD12LkS4NVQ6KM7:TR?= NUHmUIxuW0GQR1XS
LOUCY M2q5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXyTWM2OD12LkS4OFMzKM7:TR?= NEnXdpFUSU6JRWK=
NCI-H69 NUjWWng6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDpcGRKSzVyPUSuOVE4QTNizszN NELYeIpUSU6JRWK=
SCC-9 NHzlcWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHGxfWhKSzVyPUSuOVMyPzJizszN NV7DeoZPW0GQR1XS
NCI-H526 M2DTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjCcHFKSzVyPUSuOVkzQTNizszN MVTTRW5ITVJ?
NCI-H2170 NGHj[nlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTRwNk[3O|Eh|ryP M4\CXnNCVkeHUh?=
SR NEPLWpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rwNGlEPTB;ND63NFA1QCEQvF2= M4Dtb3NCVkeHUh?=
CMK MmTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWn4NHdJUUN3ME20MlczOTBzIN88US=> M3e5TXNCVkeHUh?=
COLO-829 NX\1cpNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTRwN{ewOFMh|ryP M4rQbXNCVkeHUh?=
HuO-3N1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTRwOEOyPFEh|ryP NFP6UoJUSU6JRWK=
5637 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfNTGtKSzVyPUSuPVA1QDdizszN NH7ZfVNUSU6JRWK=
A253 M4rMPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP4ZXVbUUN3ME20Mlk4PzB6IN88US=> Mn7BV2FPT0WU
NB10 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDiXIlKSzVyPUWuNFc1QTdizszN MWHTRW5ITVJ?
SF539 NUTJW3B7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTsVZdKSzVyPUWuNFk6PTlizszN M1TyRXNCVkeHUh?=
HAL-01 NG\kPXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTVwMUS2OFUh|ryP MVXTRW5ITVJ?
MHH-ES-1 M{LqUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7yboxTUUN3ME21MlE3QTJ3IN88US=> NGL5Um5USU6JRWK=
DEL MoftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUO2V3B{UUN3ME21MlI4PTh{IN88US=> MVHTRW5ITVJ?
NCI-H1299 M4Pab2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTVwM{WwNFch|ryP MUHTRW5ITVJ?
ChaGo-K-1 NUCxPGpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\NWGlEPTB;NT6zOVExPyEQvF2= MnvJV2FPT0WU
HMV-II NXe1eXZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTVwM{m0N{DPxE1? NH7RRoZUSU6JRWK=
NB69 MkLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4T5fGlEPTB;NT6zPVY{OSEQvF2= NVXuWlBFW0GQR1XS
NCI-H1882 M{S1SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTVwNEOzOlQh|ryP MYTTRW5ITVJ?
SNU-475 NWLkXWp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LyPWlEPTB;NT60O|E4OSEQvF2= NVfydHhlW0GQR1XS
RXF393 M3zROWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnzW|MyUUN3ME21MlQ5PDl2IN88US=> MnLtV2FPT0WU
CAL-51 M4XiUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjvdZozUUN3ME21MlYzQDV|IN88US=> MoXPV2FPT0WU
SW1573 NUW0T|dyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrUXYVKSzVyPUWuOlM2OzRizszN MUXTRW5ITVJ?
GCT NXS5SXZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD4TWM2OD13Lke1PVI6KM7:TR?= MnyxV2FPT0WU
COR-L88 M4C1c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1P3UGlEPTB;NT63Olg1PiEQvF2= MW\TRW5ITVJ?
MDA-MB-134-VI NFPBfW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\KO3Q4UUN3ME21Mlg4PTN4IN88US=> MmrXV2FPT0WU
NB5 MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3SOFhKSzVyPUWuPVI1PCEQvF2= M4mzbnNCVkeHUh?=
GMS-10 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHoTWM2OD13Lkm2PFYyKM7:TR?= MmrIV2FPT0WU
CHP-212 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XK[GlEPTB;Nj60PFI3PyEQvF2= M16ybnNCVkeHUh?=
TE-11 NY\tZWt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYS5cHJPUUN3ME22MlU2OTh{IN88US=> NUCw[mw2W0GQR1XS
SW962 NFXIXZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTZwNkW3O|Qh|ryP M{izPHNCVkeHUh?=
MZ2-MEL MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPxNFhxUUN3ME22MlgzODFzIN88US=> NH3NR|VUSU6JRWK=
C-33-A MoLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfQTWM2OD14LkmxOlg5KM7:TR?= NX31[404W0GQR1XS
IGR-1 NYTvc2g4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NED3S5JKSzVyPU[uPVc5OjZizszN M3HyZnNCVkeHUh?=
MOLT-4 NUTwO5VMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPwSWtKSzVyPUeuNVU1ODZizszN MnHTV2FPT0WU
NCI-H1650 MkPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXyTWM2OD15LkK3NFQ3KM7:TR?= MWPTRW5ITVJ?
AsPC-1 M3H4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHKTWM2OD15LkK4OlA2KM7:TR?= MYrTRW5ITVJ?
SNU-C2B NYPx[4E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTdwMkm1O|Eh|ryP M1[3cXNCVkeHUh?=
MKN7 NYj2U3M6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTdwM{eyN|Uh|ryP NVf1blVbW0GQR1XS
SW620 NYGwVoRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHuycWxKSzVyPUeuN|gzODVizszN Mki1V2FPT0WU
SK-MEL-28 NXTxe4dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zzZWlEPTB;Nz60NFc6QCEQvF2= M2LxOnNCVkeHUh?=
TE-6 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nwN2lEPTB;Nz60OFkxQCEQvF2= NHLHSZVUSU6JRWK=
D-263MG MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTdwNEW3OlIh|ryP MkfZV2FPT0WU
NCI-H1355 NFzOWlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTdwN{ewNlkh|ryP MVzTRW5ITVJ?
DSH1 MmDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTdwN{m3OlIh|ryP Mo\BV2FPT0WU
NCI-H460 NYfLUVJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;RdlZKSzVyPUiuNFA3QTRizszN MWTTRW5ITVJ?
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KINGS-1 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;MPZNJUUN3ME2xOk45Ojd|IN88US=> M4LSS3NCVkeHUh?=
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CAL-33 MlrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm5OGhZUUN3ME2xPE4zPzhzIN88US=> M{TCbnNCVkeHUh?=
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NCI-H650 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHRZo1IUUN3ME2xPU42QDl7IN88US=> MWnTRW5ITVJ?
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U251 NF3HPIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJ2LkC2Olgh|ryP NIP6[nJUSU6JRWK=
LoVo Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTJ2LkmyPFIh|ryP NX3wUmNGW0GQR1XS
GCIY M2TiRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJ3LkK4O|ch|ryP MoG1V2FPT0WU
NUGC-3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;TTWM2OD1{NT6zN|E3KM7:TR?= M4HENXNCVkeHUh?=
LNCaP-Clone-FGC MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkOzTWM2OD1{NT6zOFk5KM7:TR?= MXHTRW5ITVJ?
PA-1 NXu5WVA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu1Ro5KSzVyPUK1MlY5OzNizszN MVvTRW5ITVJ?
OE33 NWHYNYtpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfwc5dKSzVyPUK1MlY5PTNizszN M2nETHNCVkeHUh?=
HT-29 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTJ3Lke4O|kh|ryP NGruTYhUSU6JRWK=
RCM-1 NVfL[HhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;uS2lEPTB;MkWuPVY2PiEQvF2= MnS4V2FPT0WU
NCI-H1522 Ml7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NECzXmJKSzVyPUK1Mlk6OTFizszN NEHYcWJUSU6JRWK=
LB373-MEL-D M2fYXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon6TWM2OD1{Nj6xO|A5KM7:TR?= NGLxbHFUSU6JRWK=
NCI-H1436 NHzid3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrZPJlKSzVyPUK2MlI4OzhizszN M4PGXHNCVkeHUh?=
COLO-824 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJ4LkSwNFIh|ryP MV\TRW5ITVJ?
CP50-MEL-B M3zKTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELXSpJKSzVyPUK2MlU3PzVizszN MVrTRW5ITVJ?
EGI-1 NYTNXGt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlmwTWM2OD1{Nz6yOlk5KM7:TR?= NVXmV2FDW0GQR1XS
LAN-6 M4jkWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHrZ|VKSzVyPUK3MlM2QThizszN MmrxV2FPT0WU
GAK NEW5SHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljHTWM2OD1{Nz60NlI2KM7:TR?= NFuxU2tUSU6JRWK=
MDA-MB-175-VII MkLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJ5LkWwOVMh|ryP M4KyWnNCVkeHUh?=
JVM-2 NIjVXoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvjNXlKSzVyPUK3MlY3OjJizszN NIPiW5lUSU6JRWK=
UACC-257 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXYTWM2OD1{Nz62PFc5KM7:TR?= MXTTRW5ITVJ?
SW1783 NHrvUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvyTWM2OD1{Nz63O|g{KM7:TR?= MVzTRW5ITVJ?
HT-3 M4LSPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HtSWlEPTB;MkiuNlE3PiEQvF2= NVXOO2YzW0GQR1XS
RL MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXETWM2OD1{OD61PVEyKM7:TR?= MV3TRW5ITVJ?
TK10 NEfOZ2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJ6Lk[1N|Uh|ryP NHLKV2NUSU6JRWK=
HT55 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjVVHlKSzVyPUK5MlA2PjVizszN MWLTRW5ITVJ?
BT-20 M1PGS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInwNplKSzVyPUK5MlA2QDZizszN MVHTRW5ITVJ?
TGBC24TKB MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe1XpZwUUN3ME2yPU4yQDNzIN88US=> NWS0bJVoW0GQR1XS
HSC-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\SUGlEPTB;MkmuN|AxOSEQvF2= M2ntN3NCVkeHUh?=
COLO-205 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInWR3pKSzVyPUK5MlM6PDRizszN M4HKe3NCVkeHUh?=
GT3TKB M1nWTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HzfWlEPTB;MkmuOlg4PyEQvF2= MlXWV2FPT0WU
T47D NX3xUJcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmD3TWM2OD1{OT64OVgzKM7:TR?= NWD2UWx6W0GQR1XS
OMC-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTNyLkG5NVkh|ryP M4PrXHNCVkeHUh?=
PFSK-1 NWO4UVJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTNzLkK2OVkh|ryP NVi4SFdLW0GQR1XS
JEG-3 MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r5T2lEPTB;M{GuN|U3OSEQvF2= MX;TRW5ITVJ?
RD MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzuTWM2OD1|MT61NVE2KM7:TR?= NWn4[ogzW0GQR1XS
NCI-H64 MlvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj4T2hJUUN3ME2zNk41OTd7IN88US=> MkPzV2FPT0WU
DMS-114 NGXxW2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LYeGlEPTB;M{KuOFE5OiEQvF2= NYLMO|kyW0GQR1XS
NCI-H661 M37lfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jYOmlEPTB;M{KuOlUxOSEQvF2= NX7rNWZ1W0GQR1XS
CAL-148 NHflS4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rPPWlEPTB;M{KuOlY3PSEQvF2= NV64Wm4yW0GQR1XS
HuP-T3 NWLKZowyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTN{LkmzN|gh|ryP NVTodW9{W0GQR1XS
ES4 NWe5U2c{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1[4XmlEPTB;M{OuNVcxPSEQvF2= MWnTRW5ITVJ?
Ca9-22 M16xU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vHTmlEPTB;M{OuOFYxOSEQvF2= NFjXPItUSU6JRWK=
LP-1 NF7OcnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfBUW5[UUN3ME2zOE4xQSEQvF2= MUnTRW5ITVJ?
AU565 NEHZdmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPYS5RYUUN3ME2zOE42ODZ7IN88US=> MlzIV2FPT0WU
MDA-MB-453 NHLicI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DuN2lEPTB;M{WuNVQzPiEQvF2= MnKwV2FPT0WU
SNU-C1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTN3LkG3NUDPxE1? M1TtRXNCVkeHUh?=
SW13 NE[xTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTN3LkSwO|Yh|ryP M1Po[3NCVkeHUh?=
NCI-H2122 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELvdmVKSzVyPUO1MlU2QThizszN Ml7IV2FPT0WU
NCI-H1395 NH3VN5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLWboNKSzVyPUO1MlY3QTFizszN M3vWb3NCVkeHUh?=
J-RT3-T3-5 NY\h[nBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzUSHBqUUN3ME2zOk4xOjl2IN88US=> MoPSV2FPT0WU
COR-L279 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnW4TWM2OD1|Nj6xPVgyKM7:TR?= M4nncnNCVkeHUh?=
ATN-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTMflY5UUN3ME2zOk45PTF4IN88US=> MVvTRW5ITVJ?
HCC2998 NHvET3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PrZmlEPTB;M{[uPFU4OSEQvF2= NIm1XVBUSU6JRWK=
UM-UC-3 MoTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\3ZnF4UUN3ME2zOk45Pjd3IN88US=> M{XtUnNCVkeHUh?=
DV-90 MoTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTN4LkmwOlch|ryP NXTTPW9wW0GQR1XS
ES8 MoHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrqUJJLUUN3ME2zOk46OzF6IN88US=> MV7TRW5ITVJ?
YAPC M3XROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU[1UZRNUUN3ME2zOk46PjV2IN88US=> NIrmSnVUSU6JRWK=
HCC1599 M13jc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUW4R45yUUN3ME2zO{4yPjF6IN88US=> MmnCV2FPT0WU
UMC-11 M37zN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTN5LkK1NFMh|ryP NHSxTmJUSU6JRWK=
THP-1 M4rtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfwNWFQUUN3ME2zO{4zQDZ6IN88US=> MWLTRW5ITVJ?
OCUB-M M4TmN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrxTWM2OD1|Nz6yPFkyKM7:TR?= MV\TRW5ITVJ?
NCI-H1693 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTN5LkOyN|Mh|ryP NF7nb3RUSU6JRWK=
NCI-H345 NH7oZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHu0O4pKSzVyPUO3MlM3OjRizszN M2fsZnNCVkeHUh?=
COLO-800 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nTbGlEPTB;M{euOVY4KM7:TR?= M3TTbHNCVkeHUh?=
COLO-320-HSR NF6yWHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTN6LkO0PVIh|ryP NVOyVndTW0GQR1XS
NCI-H596 M2GySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTN6LkS0PFkh|ryP NHW4XmxUSU6JRWK=
NCI-H187 Mo\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13nWGlEPTB;M{iuO|M1PCEQvF2= MVfTRW5ITVJ?
ECC4 MojyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nQcGlEPTB;M{muNFgyPCEQvF2= MnHRV2FPT0WU
KP-4 NEfvW4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXHbnVoUUN3ME2zPU4yOjN3IN88US=> M{DBVXNCVkeHUh?=
NCI-H2227 NHjCNVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPQSXlKSzVyPUO5MlM6PDlizszN NH7LSWxUSU6JRWK=
22RV1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGq4[nlKSzVyPUO5Mlg{QThizszN MYnTRW5ITVJ?
SAS MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf5NY9KSzVyPUSwMlA6PiEQvF2= NVfMNnp4W0GQR1XS
PANC-10-05 MkfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnje2RQUUN3ME20NE4yQDJ6IN88US=> MWjTRW5ITVJ?
MDA-MB-468 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjRTWM2OD12MD61N|Q3KM7:TR?= M{Ta[3NCVkeHUh?=
RPMI-7951 NH3RVGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmw[GJKSzVyPUSxMlIxPzVizszN NFzPZY5USU6JRWK=
BB49-HNC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13pdmlEPTB;NEGuNlE4QSEQvF2= NHnRZZRUSU6JRWK=
23132-87 M{fQZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX1SXdKSzVyPUSxMlI4OzJizszN NF;FclNUSU6JRWK=
HCC1569 M3LNSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zaZ2lEPTB;NEGuNlg5PSEQvF2= NFv2WGtUSU6JRWK=
CP66-MEL MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTR{LkG4PFYh|ryP NFWzcW5USU6JRWK=
K-562 M{TPdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfZbIpKSzVyPUSyMlI5PTRizszN NGDsNoNUSU6JRWK=
OCI-AML2 NEHDWmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDwS4JKSzVyPUSyMlg6PzRizszN NIXQeo9USU6JRWK=
SW756 NEDabG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXsfopLUUN3ME20N{4xOzh6IN88US=> NGHQeotUSU6JRWK=
M14 M2HSdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHzbWZKSzVyPUSzMlMyQDlizszN MmqwV2FPT0WU
NCI-H1623 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPnNlJjUUN3ME20N{41PjRizszN MXLTRW5ITVJ?
KNS-81-FD NXLUeFBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWr2UXl5UUN3ME20N{44PjJizszN M{fRXHNCVkeHUh?=
TGBC1TKB NEO5U5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nZRWlEPTB;NEOuPVA6QSEQvF2= MofiV2FPT0WU
RERF-LC-MS NGHMOo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDZOoFKSzVyPUSzMlkzQDFizszN NV70eJg4W0GQR1XS
PC-3 NU\qT3pxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrC[oNrUUN3ME20OE41OzR5IN88US=> M334NHNCVkeHUh?=
HuP-T4 M4GwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnvd2dyUUN3ME20OE41PDd2IN88US=> NXj5ephNW0GQR1XS
NCI-H510A MoewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTR2LkewPEDPxE1? M4nQSXNCVkeHUh?=
LB2518-MEL NFfGNVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLCTWM2OD12ND63PVM4KM7:TR?= NIXWTo1USU6JRWK=
TE-5 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTR3Lkm1PFEh|ryP M4XaTHNCVkeHUh?=
EW-24 NYPkS|JKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTR4LkG3NlMh|ryP NV:3S|RtW0GQR1XS
LB647-SCLC NXXpfHNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzMTWM2OD12Nj6yNVU2KM7:TR?= NWWy[FdWW0GQR1XS
NCI-H524 NIPKPINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILzcJlKSzVyPUS2MlcyQDVizszN MU\TRW5ITVJ?
EW-11 MonES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3hPGtyUUN3ME20Ok46Ozd|IN88US=> MkLHV2FPT0WU
KALS-1 M3vmV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nNW2lEPTB;NEeuNlA3PiEQvF2= NFPYO4lUSU6JRWK=
BT-474 NWTnRXQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7H[JBKSzVyPUS3MlQzOTZizszN NGTtcFVUSU6JRWK=
SK-N-AS NF3BSZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTR5Lki4PEDPxE1? M1j2dXNCVkeHUh?=
HCC2157 MlTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3O0dmlEPTB;NEiuNFc3KM7:TR?= MVzTRW5ITVJ?
HCC1954 MoTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrkTWM2OD12OD6xO|A1KM7:TR?= M{TWeXNCVkeHUh?=
FADU M4jjSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvkUXBKSzVyPUS4MlMxOzFizszN NHjYd3pUSU6JRWK=
S-117 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmWzTWM2OD12OD6zPFE2KM7:TR?= M{frVHNCVkeHUh?=
LS-1034 MmHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTR6LkewOlch|ryP MnSyV2FPT0WU
CAMA-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH1VppKSzVyPUS5MlU2PDNizszN NG\yVJdUSU6JRWK=
LU-134-A NV3rR5FXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfRfnJnUUN3ME20PU45ODh3IN88US=> Mln0V2FPT0WU
NCI-H1838 NIT3UG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;OXXpKSzVyPUS5MlgxQDdizszN NVPzXoY2W0GQR1XS

... 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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