Axitinib

Licensed by Pfizer Catalog No.S1005 Synonyms: AG 013736

Axitinib Chemical Structure

Molecular Weight(MW): 386.47

Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

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Cited by 38 Publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
Features Superior as second-line therapy relative to sorafenib (current standard-of-care).
Targets
VEGFR1/FLT1 [1]
(Porcine aorta endothelial cells)
VEGFR2/Flk1 [1]
(Porcine aorta endothelial cells)
VEGFR2/KDR [1]
(Porcine aorta endothelial cells)
VEGFR3 [1]
(Porcine aorta endothelial cells)
PDGFRβ [1]
(Porcine aorta endothelial cells)
0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM 1.6 nM
In vitro

Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC). [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell M4HLc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4S5SGlEPTB;MD6wNFAxPTF|IN88US=> MnTRV2FPT0WU
NCI-H1703 NED6O4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHZTWM2OD1yLkCwNFkxOiEQvF2= MXnTRW5ITVJ?
KASUMI-1 M4L0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vCOWlEPTB;MD6wNFY5OiEQvF2= MUnTRW5ITVJ?
CGTH-W-1 NVi3V3R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTBwMEC3NlIh|ryP M{f6OHNCVkeHUh?=
A204 M3ziUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDvUHVKSzVyPUCuNFA6QTJizszN MV3TRW5ITVJ?
HOP-62 M{DNNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfRTWM2OD1yLkGwPFM3KM7:TR?= Mk\KV2FPT0WU
H-EMC-SS Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwMUGwNFUh|ryP NIexW|hUSU6JRWK=
KU812 NEjxeYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwMU[1O|ch|ryP MV7TRW5ITVJ?
EM-2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwMU[4NVYh|ryP NXric5lKW0GQR1XS
LAMA-84 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi0TWM2OD1yLkG3OlY2KM7:TR?= MUfTRW5ITVJ?
JAR NUHLd25yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r3TWlEPTB;MD6yN|k5QSEQvF2= NYjNeHdIW0GQR1XS
G-361 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HlVWlEPTB;MD6zNlMzPSEQvF2= NFr5SYVUSU6JRWK=
KG-1 MkfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrmTWM2OD1yLkO3OlQzKM7:TR?= NFfGVpBUSU6JRWK=
BV-173 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwM{mzNkDPxE1? Ml24V2FPT0WU
K5 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnBTWM2OD1yLkSyNVI4KM7:TR?= NEPBZXNUSU6JRWK=
MEG-01 NUHtcFZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v5VmlEPTB;MD60NlM3OSEQvF2= NHvs[YJUSU6JRWK=
MFM-223 NXX3UIV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNES3O|Yh|ryP M2jRXnNCVkeHUh?=
BE-13 NHfPZodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTBwNUGwNFgh|ryP MnHIV2FPT0WU
NEC8 M1PaUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPa[IVKSzVyPUCuO|IyOTNizszN M1faenNCVkeHUh?=
SW756 NFy1WGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zINGlEPTB;MD65PVg1PiEQvF2= NFq4R4ZUSU6JRWK=
A2780 M1LnVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofJTWM2OD1zLkCxNVQ3KM7:TR?= MXfTRW5ITVJ?
NB14 MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzuS4FlUUN3ME2xMlAyQDBzIN88US=> NH3UbYVUSU6JRWK=
H4 MljRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTFwME[0NlIh|ryP NH7jSJJUSU6JRWK=
SK-OV-3 M{Tl[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFwME[2N|Mh|ryP Mmn2V2FPT0WU
AN3-CA Mki5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7jZY5IUUN3ME2xMlA5Ozh7IN88US=> NIXhO4dUSU6JRWK=
A427 NUPXd3RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHYR2ZKSzVyPUGuNVA{QDFizszN MkHjV2FPT0WU
ES7 Ml;BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLuTWM2OD1zLkGxN|M1KM7:TR?= MnPFV2FPT0WU
AGS NF;ld|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITDO3NKSzVyPUGuNVE{QTVizszN MVzTRW5ITVJ?
G-402 MoHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rpTGlEPTB;MT6xOFY6PCEQvF2= NE\qfYZUSU6JRWK=
ES5 NXe2XJN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17tS2lEPTB;MT6xO|I1QCEQvF2= NGnmb3JUSU6JRWK=
DEL NXHEU5V4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVG5WldCUUN3ME2xMlI2PDV5IN88US=> MnPOV2FPT0WU
NB10 MoD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFwM{K1OVch|ryP MV7TRW5ITVJ?
NCI-H1581 NX;CclZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnD[HBKSzVyPUGuN|kxPDJizszN M1vJcHNCVkeHUh?=
D-566MG NEXpNHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXLfpBKSzVyPUGuOFA3QDNizszN NVLkfIw5W0GQR1XS
LXF-289 MojBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;We4FpUUN3ME2xMlQ{QTl4IN88US=> NWDze2FRW0GQR1XS
BT-549 NHLUdZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3O0eWlEPTB;MT61OlkxQSEQvF2= MUXTRW5ITVJ?
NKM-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXuTmVKSzVyPUGuOlA2PTZizszN NILVWlRUSU6JRWK=
SW780 NFzBWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFwNkWxOVgh|ryP MW\TRW5ITVJ?
NCI-H292 NELOTY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHlTWM2OD1zLk[2N|g{KM7:TR?= MVzTRW5ITVJ?
HMV-II NEDGdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D0cGlEPTB;MT63NFQ5QCEQvF2= NGjMVmlUSU6JRWK=
ALL-PO NHrSVlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjY[IM5UUN3ME2xMlgxODF3IN88US=> MlPEV2FPT0WU
UACC-257 MnfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUO0NZo{UUN3ME2xMlgzOTZ|IN88US=> NXSyTYl3W0GQR1XS
PA-1 NW\KXmFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf6emtKSzVyPUGuPFI4OjVizszN NYLIeWl{W0GQR1XS
HD-MY-Z NGH1SFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX6wXGdIUUN3ME2xMlg3OjhzIN88US=> M4mxR3NCVkeHUh?=
HSC-4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCzTWM2OD1zLkmzPFM6KM7:TR?= MlnsV2FPT0WU
GCT NEP3W2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NICyZVZKSzVyPUKuNFA6OTZizszN M1e5cXNCVkeHUh?=
RT-112 MnzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DmVGlEPTB;Mj6xN|QzPCEQvF2= M3rK[XNCVkeHUh?=
A172 M1e4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\WOGlEPTB;Mj6xN|YxPiEQvF2= NW\NT5ZpW0GQR1XS
HCE-T NI\RfHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\h[3JKSzVyPUKuNlA2QThizszN NUSzfIJTW0GQR1XS
YH-13 M171S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjNTWM2OD1{LkKxOlcyKM7:TR?= MVfTRW5ITVJ?
DK-MG NWnkTo5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJwMkO4N|Qh|ryP NV\YOZh3W0GQR1XS
ACN M1PDTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjOTWM2OD1{LkKzPFc2KM7:TR?= MVjTRW5ITVJ?
VA-ES-BJ MoG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1eydmlEPTB;Mj6yOFk2PyEQvF2= MVTTRW5ITVJ?
L-363 M1G5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rQTGlEPTB;Mj6yPFA3OSEQvF2= NIrWO3FUSU6JRWK=
HuH-7 NGfTcYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\1XmlKSzVyPUKuOFIyPjVizszN NFHyO2lUSU6JRWK=
A4-Fuk NGKzdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7WTWM2OD1{LkS3NVY5KM7:TR?= NUL1cYY1W0GQR1XS
T-24 NYT4O3NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLBTWM2OD1{LkS4NFM4KM7:TR?= Mn;jV2FPT0WU
GOTO MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJwNUOwNVMh|ryP MYnTRW5ITVJ?
MV-4-11 M1rtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jPZWlEPTB;Mj61PVE3QSEQvF2= M4PJRnNCVkeHUh?=
DMS-114 NWHGfld2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnYWFNoUUN3ME2yMlY3OzR3IN88US=> NWXoUFdzW0GQR1XS
MHH-NB-11 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJwN{CyPVkh|ryP MXPTRW5ITVJ?
CHP-212 M4Lpc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;oeXVZUUN3ME2yMlgzODlzIN88US=> NGDSW4FUSU6JRWK=
DMS-273 M{WxN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlH0TWM2OD1{LkmwNlA4KM7:TR?= MnvCV2FPT0WU
SF295 NVjQNVVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTNwMEK1PVch|ryP NX7EPHQ{W0GQR1XS
NCI-H1563 NI\2OmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTNwMUWwNFUh|ryP NIf1T5RUSU6JRWK=
NCI-H446 M17qSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rSRmlEPTB;Mz6yNlgxPSEQvF2= MXfTRW5ITVJ?
HCC1806 MnnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXyTWM2OD1|LkK3OlU4KM7:TR?= MV7TRW5ITVJ?
SF126 NIDCSpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[wSWhKSzVyPUOuN|AxOTdizszN MoLMV2FPT0WU
SW982 M1vnW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTNwM{O4O|Uh|ryP MXvTRW5ITVJ?
ES8 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjKe4VvUUN3ME2zMlM1QTl7IN88US=> NFHleYVUSU6JRWK=
SCC-4 NFzvN21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrQcGJJUUN3ME2zMlUxOzl4IN88US=> Mk\4V2FPT0WU
RPMI-8226 MlzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnKN|FuUUN3ME2zMlYzPjF4IN88US=> MlS5V2FPT0WU
EW-11 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4m5TmlEPTB;Mz62N|AzOiEQvF2= NGjFWnRUSU6JRWK=
COR-L105 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\TcpNKSzVyPUOuOlM{OzRizszN NHL0[I9USU6JRWK=
ES1 NYPHXXdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTNwOEOwPVQh|ryP NXm5O3prW0GQR1XS
KMOE-2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\kZmlEPTB;Mz65NVgxQCEQvF2= M3zZSXNCVkeHUh?=
ABC-1 Mn3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnocZNvUUN3ME2zMlk{QTFzIN88US=> M3rJNXNCVkeHUh?=
NCI-H526 M3rhcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1e0UmlEPTB;Mz65PVEzPiEQvF2= NVHPSZRsW0GQR1XS
HCC1395 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TrdGlEPTB;Mz65PVQ5PCEQvF2= NHjrNWlUSU6JRWK=
DU-145 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NISzcZVKSzVyPUSuNVI5OjVizszN NW\xd3N6W0GQR1XS
JEG-3 Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnwTWM2OD12LkG1PVE3KM7:TR?= MU\TRW5ITVJ?
HCC1187 MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq0VYFWUUN3ME20MlIyPTl5IN88US=> NF:3TVhUSU6JRWK=
LC-2-ad MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLSfZk5UUN3ME20MlIzOTd5IN88US=> NEjCWVNUSU6JRWK=
ONS-76 NV;RflF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfiTWM2OD12LkK0NVkzKM7:TR?= MWfTRW5ITVJ?
CAL-27 M{PiWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYmwbHd4UUN3ME20MlI1OzR2IN88US=> NI\QXIFUSU6JRWK=
8-MG-BA NHuwSVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVX1VVlFUUN3ME20MlI3PjV6IN88US=> NXXlSog5W0GQR1XS
HGC-27 M2XFZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDrd2FKSzVyPUSuNlk3PiEQvF2= MX3TRW5ITVJ?
Hs-578-T M3Pncmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXflXHk1UUN3ME20MlMyPDZ6IN88US=> MmHuV2FPT0WU
EW-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfDXm9KSzVyPUSuOVMxOTRizszN NED1d5dUSU6JRWK=
SW1573 NHfrfoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTRwNUWxOlMh|ryP NU\GcWJMW0GQR1XS
SNU-423 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17kcWlEPTB;ND62NFc6KM7:TR?= MlfEV2FPT0WU
HOS NVr3W3NHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTRwNkm3O{DPxE1? M1[5UHNCVkeHUh?=
LB1047-RCC M1S3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzUTWM2OD12LkixOFE5KM7:TR?= Mlf1V2FPT0WU
ChaGo-K-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXDNIxKSzVyPUSuPFkxPDhizszN M3TIOXNCVkeHUh?=
A3-KAW NVrjVHhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\aTWM2OD12Lkm3N|UzKM7:TR?= NX\BdpRQW0GQR1XS
CAS-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTRwOUm5NFgh|ryP MljtV2FPT0WU
NBsusSR NWXKSpBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnO3TWM2OD13LkCzOVE1KM7:TR?= MkHaV2FPT0WU
KM12 NFfYUVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XjUGlEPTB;NT6yPVgzPyEQvF2= MlTDV2FPT0WU
NCI-H1155 M1S5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O1ZmlEPTB;NT6zPFE5PSEQvF2= M3vvfnNCVkeHUh?=
EFM-19 NWTkVm9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X2T2lEPTB;NT60NVc{PyEQvF2= NE\TVmZUSU6JRWK=
D-392MG M17OSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP0WIhKSzVyPUWuOVc5PDlizszN Mnf4V2FPT0WU
JVM-3 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTVwN{KzNlUh|ryP NVTISVRVW0GQR1XS
EW-16 MlXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1GzOWlEPTB;NT63OVU5OyEQvF2= NHfie3dUSU6JRWK=
KARPAS-45 Mo\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zjOGlEPTB;NT64OFMzPSEQvF2= MWXTRW5ITVJ?
NCI-H28 NUDDR3NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTVwOEe5NVgh|ryP NEfrOFNUSU6JRWK=
COLO-829 MnfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXsTWM2OD13LkmxOVA1KM7:TR?= NXPvfG8xW0GQR1XS
KM-H2 NF:wUlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTVwOUKzPVUh|ryP NV;MPHhpW0GQR1XS
NCI-H82 M1X3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HrWWlEPTB;NT65Nlc4OSEQvF2= NFr2TFZUSU6JRWK=
OAW-42 MljzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfSTWM2OD13Lkm4PFIyKM7:TR?= MnfVV2FPT0WU
A704 NI\6[WFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTZwMUC1O|Qh|ryP NVftdpVkW0GQR1XS
NCI-H1048 Mkf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnkZoZWUUN3ME22MlExPTl7IN88US=> NIHuT|FUSU6JRWK=
LOXIMVI MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDuTWM2OD14LkGxNlQ5KM7:TR?= M2HNenNCVkeHUh?=
MKN45 NU\t[mhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTZwMk[wNVYh|ryP NUG4b5ZEW0GQR1XS
D-502MG M370c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rrdGlEPTB;Nj6yPFg2PyEQvF2= M4fPXnNCVkeHUh?=
HUTU-80 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTZwNEG2PFgh|ryP NWDDXHB3W0GQR1XS
S-117 NVXRUmpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXKTWM2OD14LkWwNlY4KM7:TR?= MXHTRW5ITVJ?
HCC1569 NGnlPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDqPWJ2UUN3ME22MlU{PzN5IN88US=> M1rmTnNCVkeHUh?=
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LCLC-103H NX;xSmY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLsVnVKSzVyPUKyMlQ4PTJizszN NHv5OItUSU6JRWK=
D-542MG NXrT[5YyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrYdoRKSzVyPUKyMlU2PThizszN MlrtV2FPT0WU
ATN-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD1TWM2OD1{Mj62OFM6KM7:TR?= MWnTRW5ITVJ?
SK-MEL-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXPTWM2OD1{Mj64N|Y5KM7:TR?= M{fSXnNCVkeHUh?=
HDLM-2 MlLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ|LkG0O|gh|ryP MorvV2FPT0WU
UM-UC-3 Mk\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4i3b2lEPTB;MkOuNVk1PCEQvF2= Mn3nV2FPT0WU
NCI-H1573 M{TZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7ud2hlUUN3ME2yN{41PjhzIN88US=> NEDId5pUSU6JRWK=
NCI-H520 NWrCO496T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHZTWM2OD1{Mz60PVQ5KM7:TR?= MXHTRW5ITVJ?
ESS-1 NUW3XXBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TndmlEPTB;MkOuPFA2QSEQvF2= NXTxd5BoW0GQR1XS
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TGBC24TKB MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJ2LkCzNVIh|ryP MnjTV2FPT0WU
HCC1937 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{joWGlEPTB;MkSuNUDPxE1? MWTTRW5ITVJ?
RS4-11 M{PNdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHmz[G5KSzVyPUK0MlE1OiEQvF2= NXXRdVJbW0GQR1XS
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RPMI-2650 M2PFdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVG3OoduUUN3ME2yOE43OTZ{IN88US=> M{\5c3NCVkeHUh?=
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YAPC MnnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH76NJdKSzVyPUK0MlgzOTRizszN MkjrV2FPT0WU
NB13 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\oTWM2OD1{NT6yOlEyKM7:TR?= Mm\lV2FPT0WU
SK-N-AS M{DmXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\nenBKSzVyPUK1Mlg2QDRizszN Mom4V2FPT0WU
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NCI-H810 NIDMW41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELJT|NKSzVyPUK2MlMyOTJizszN MW\TRW5ITVJ?
NCI-SNU-1 M1LW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXYTWM2OD1{Nj61OFU1KM7:TR?= M37sWnNCVkeHUh?=
HH MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC0U5hKSzVyPUK2MlU2OjlizszN MlLTV2FPT0WU
U-2-OS M{nnUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn6OGtHUUN3ME2yOk44Ozh{IN88US=> MnXYV2FPT0WU
SF539 MmfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJ4LkiwNVgh|ryP MknpV2FPT0WU
NCI-H2052 M{[0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjKOFE4UUN3ME2yO{4xQDZizszN M3rCXHNCVkeHUh?=
A673 MmK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnBNlQyUUN3ME2yO{4zOTB{IN88US=> M130dXNCVkeHUh?=
WM-115 M4nIcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHoSZlKSzVyPUK3Mlc4PjdizszN MmmyV2FPT0WU
SW48 NVnTfFlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrsTWM2OD1{Nz64NFA2KM7:TR?= MkXSV2FPT0WU
NOMO-1 M3H5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJ5Lki1N|Ih|ryP M1f0ZnNCVkeHUh?=
PC-3 M3;ydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTUVJJRUUN3ME2yO{45QTRzIN88US=> NIHHW2JUSU6JRWK=
UMC-11 M4K4Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzkTWM2OD1{Nz65N|Q{KM7:TR?= NFjR[21USU6JRWK=
U-118-MG M2PRXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlf1TWM2OD1{OD6wNVI{KM7:TR?= MnLHV2FPT0WU
NCI-H2452 M3HCZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJ6LkC4NlIh|ryP M4jCWnNCVkeHUh?=
CAMA-1 NELmfVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJ6Lki1OlQh|ryP MnO3V2FPT0WU
MC-IXC NXTme3VbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf4OZZUUUN3ME2yPU4zOzZ4IN88US=> NIS5SG1USU6JRWK=
ES4 NUfqVXg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mme4TWM2OD1{OT6zNVczKM7:TR?= MUfTRW5ITVJ?
BHT-101 NI\OO5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLhfHNKSzVyPUK5MlMzOSEQvF2= M1jCd3NCVkeHUh?=
KP-4 NFT3WXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7QZVJKSzVyPUK5MlUyPiEQvF2= NHzBfYdUSU6JRWK=
CAL-54 NETVfZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWD3T21rUUN3ME2yPU42PDR3IN88US=> NGP0bIRUSU6JRWK=
5637 NVLtell4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NICxNZpKSzVyPUK5MlY1OjFizszN M4nOenNCVkeHUh?=
MOLT-16 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTvb5ZPUUN3ME2yPU44OjZ7IN88US=> M1vXOXNCVkeHUh?=
Ca-Ski M2\uNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{D4TGlEPTB;MkmuPVQ3KM7:TR?= M4jmN3NCVkeHUh?=
AsPC-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTNyLkCyNVIh|ryP MUjTRW5ITVJ?
MSTO-211H M2e3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XNN2lEPTB;M{CuNVUh|ryP M{W4[3NCVkeHUh?=
L-428 M2C4VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PkSmlEPTB;M{CuOFA2KM7:TR?= MmjsV2FPT0WU
SW1463 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3uxUGlEPTB;M{CuOVM5OyEQvF2= NEHPU4JUSU6JRWK=
NCI-H1648 M{\k[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3CWVhKSzVyPUOwMlU2PzRizszN M3HuZXNCVkeHUh?=
CAKI-1 NH:5U4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fSNGlEPTB;M{CuO|cxOiEQvF2= Ml7mV2FPT0WU
YKG-1 NW\0S411T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIqxOGpKSzVyPUOxMlAzPjNizszN M1;UUXNCVkeHUh?=
A2058 NFOybWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWT5UoJRUUN3ME2zNU4yOTZ2IN88US=> NYG1S4EyW0GQR1XS
A375 MoHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7GTWM2OD1|MT6xOlk3KM7:TR?= M4j6b3NCVkeHUh?=
SNB75 M1HI[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTNzLkK0N|Uh|ryP NXfQdZdwW0GQR1XS
SK-HEP-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTNzLkSyO|Eh|ryP MlL6V2FPT0WU
ME-180 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TDOGlEPTB;M{GuOlU1OiEQvF2= MlqzV2FPT0WU
NCI-H209 MnfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTNzLkiyOFch|ryP MlPEV2FPT0WU
HC-1 NF;vN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDHS3pKSzVyPUOyMlE1PDZizszN NFH2SWdUSU6JRWK=
LB373-MEL-D M1PreWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvwdGJKSzVyPUOyMlE6PzFizszN NVzzNVRYW0GQR1XS
SNU-387 NF3zcG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTN{LkOxPVEh|ryP M3jsSHNCVkeHUh?=
C32 NUT0bXJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X2Z2lEPTB;M{KuN|M2OyEQvF2= M2nPbHNCVkeHUh?=
EW-13 NUnTN4xkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzwTWM2OD1|Mj65OFA5KM7:TR?= M{fJPHNCVkeHUh?=
BFTC-905 M2TJc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILqN5FKSzVyPUOzMlUyOzZizszN MnTHV2FPT0WU
NCI-H1299 M4XJbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M12w[WlEPTB;M{OuOVYzOSEQvF2= M2m0ZnNCVkeHUh?=
LU-135 NETI[29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;jSmlEPTB;M{OuPFAyKM7:TR?= NIPF[GNUSU6JRWK=
NCI-H2122 NUTSUnhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrnTWM2OD1|Mz65PVY3KM7:TR?= MWPTRW5ITVJ?
SK-LMS-1 NFPFOZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;ITWM2OD1|ND60NVA4KM7:TR?= NUXLb48{W0GQR1XS
LNCaP-Clone-FGC NIrIdHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTN2Lki1NVUh|ryP MWjTRW5ITVJ?
NCI-H1092 M{\PXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfJTWM2OD1|NT6yO|Q4KM7:TR?= NWHYXmdZW0GQR1XS
MS-1 NI\leWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrOUmJKSzVyPUO1MlMxOzhizszN M{nRU3NCVkeHUh?=
KYSE-510 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TKOWlEPTB;M{WuOVA1OiEQvF2= NGLFOmxUSU6JRWK=
NCI-H1793 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHqbm1KSzVyPUO1MlY2PDVizszN NFnROVVUSU6JRWK=
MIA-PaCa-2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTN4LkC0PVYh|ryP M4\LcXNCVkeHUh?=
EW-22 M3vnS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTN4LkSwO|Ih|ryP MYfTRW5ITVJ?
IGR-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrObmhNUUN3ME2zOk45OTh2IN88US=> MUPTRW5ITVJ?
HT-1080 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXvTWM2OD1|Nz6xNlUh|ryP MVnTRW5ITVJ?
M14 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELwfnFKSzVyPUO3MlE3PDJizszN M3[wenNCVkeHUh?=
786-0 NWHOZ2F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTN5LkK3PVQh|ryP M2r2PXNCVkeHUh?=
MZ2-MEL MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHJOGxKSzVyPUO3MlQ2ODFizszN NU\s[I9TW0GQR1XS
NCI-H510A M2j2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXsbVZKSzVyPUO3Mlk1OTJizszN MnvYV2FPT0WU
LAN-6 NGjxbYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz3TWM2OD1|Nz65OVgzKM7:TR?= M1vhcnNCVkeHUh?=
SW620 MmrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmqyTWM2OD1|OD60PVc1KM7:TR?= MlnMV2FPT0WU
LB2241-RCC MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nx[WlEPTB;M{muPFIxPSEQvF2= MmnhV2FPT0WU
Detroit562 NGXxb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTRyLkGyOlgh|ryP MojaV2FPT0WU
HN NYj4clJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFezR|RKSzVyPUSwMlE4QDJizszN NYnVeIFuW0GQR1XS
HCT-15 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ezXWlEPTB;NECuOVkxPyEQvF2= MnHWV2FPT0WU
C2BBe1 NWHXS2hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jOWGlEPTB;NECuPVE2PyEQvF2= MnPoV2FPT0WU
A498 NGXMNoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTRzLkOwNVUh|ryP M2HrbnNCVkeHUh?=
SK-MEL-24 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzDTWM2OD12MT60O|I2KM7:TR?= M3mwNXNCVkeHUh?=
OVCAR-5 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTRzLke3Olch|ryP NY\T[255W0GQR1XS
NCI-H1792 MlPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjiTWM2OD12MT65PFIyKM7:TR?= MmLxV2FPT0WU
KOSC-2 NIG2[nRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTR{LkK2PVkh|ryP NXT5coZZW0GQR1XS
Mo-T NWfkXGJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDZTWM2OD12Mj64PVU5KM7:TR?= NVnlbWpNW0GQR1XS
CFPAC-1 NX:4dHppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHHTWM2OD12Mz60PVQ1KM7:TR?= M3zhb3NCVkeHUh?=
CAL-51 NFfFcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ezbWlEPTB;NEOuOVYxPSEQvF2= NYDBOnlRW0GQR1XS
RH-18 MmjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGq1TJJKSzVyPUSzMlgxPSEQvF2= M2T4WHNCVkeHUh?=
EC-GI-10 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;QTWM2OD12Mz64N|Q4KM7:TR?= MnrqV2FPT0WU
HSC-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PFT2lEPTB;NESuNFA6KM7:TR?= NVX6do9ZW0GQR1XS
ML-2 NX7ETYwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3:ydmlEPTB;NEWuNlYzOSEQvF2= NUDMfmxSW0GQR1XS
KNS-81-FD MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DyZmlEPTB;NEWuO|M3PSEQvF2= M3j6dXNCVkeHUh?=
NB6 M{S3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWG0cno6UUN3ME20Ok4yOTFizszN MYnTRW5ITVJ?
MCF7 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\3XWlEPTB;NE[uOVU{OyEQvF2= NVLISFMzW0GQR1XS
P30-OHK Ml\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLzSHE{UUN3ME20Ok45OTF5IN88US=> Mn20V2FPT0WU
BPH-1 NUPlUI9JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[5TWM2OD12Nj65PFA2KM7:TR?= NF;DcFBUSU6JRWK=
U251 M1e0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7zSmxzUUN3ME20Ok46QTRizszN NF3IRYRUSU6JRWK=
MKN1 NFnRPXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DscWlEPTB;NEeuOVE{PyEQvF2= M1:1[XNCVkeHUh?=
A431 M4f4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HBPGlEPTB;NEeuPFM{QCEQvF2= MkTLV2FPT0WU
C8166 MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XlS2lEPTB;NEmuNlA{QSEQvF2= MoTHV2FPT0WU
HEL M1X6O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHkdGFDUUN3ME20PU41ODZ2IN88US=> NFu1NI5USU6JRWK=
RMG-I NXy0TnlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVG0fIN[UUN3ME20PU41PDR2IN88US=> MofQV2FPT0WU
CAL-72 M3H2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD3TWM2OD12OT62NFc2KM7:TR?= M{fjOnNCVkeHUh?=
SW962 MkflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\j[ZVKSzVyPUS5Mlk{OzJizszN M1j0W3NCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-c-kit / c-kit / p-AKT / AKT / p-ERK / ERK / p-STAT3 / STAT3 / p-STAT5 / STAT5 / p-S6K / S6K / p-S6 / S6; 

PubMed: 31205508     


Immunoblotting analysis of indicated proteins in c-KIT mediated signaling pathways of GIST-T1, GIST-882, GIST-48B, and GIST-5R cell lines.

PARP / cleaved PARP / caspase-3 / cleaved caspase-3; 

PubMed: 31205508     


Immunoblotting analysis of apoptosis-related proteins after axitinib treatment in human GIST cell lines. Imatinib and sunitinib were used as positive controls.

31205508
Immunofluorescence
alpha-tubulin; 

PubMed: 26474283     


Representative images of RCC cells treated as above described, and then immunostained with anti-α-tubulin antibody. Bar: 50 μM

26474283
Growth inhibition assay
Cell viability ; 

PubMed: 26474283     


A. A-498 and Caki-2 RCC cell lines were cultured up to 96 h with different doses of axitinib. Cell viability was determined by MTT assay. Data shown are expressed as mean ± SD of three separate experiments; *p < 0.01 vs vehicle-treated cells. B. RCC cell 䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ ⟸෕Ð㺣痖⟸෕€

26474283
In vivo Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). [1] Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. [2] Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. [3] Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.

Protocol

Kinase Assay:

[1]

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Cellular receptor kinase phosphorylation assay:

Porcine aorta endothelial (PAE) cells, which overexpress full-length VEGFR2, PDGFRβ, Kit, and NIH-3T3, which overexpress murine VEGFR2 (Flk-1) or PDGFRα, are generated. The 96-well plates are coated with 100 μL/well of 2.5 μg/mL anti-VEGFR2 antibody, 0.75 μg/mL anti-PDGFRβ antibody, 0.25 μg/mL anti-PDGFRα antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody to prepare ELISA capture plates. Then phosphorylation of RTK is measured by ELISA.
Cell Research:

[2]

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  • Cell lines: HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cells
  • Concentrations: 1 nM - 10 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are seeded in a 96-well plate at a density of 5 × 104 and cultured for 24 hours. Axitinib is added to the cells at concentrations ranging from 1 nM to 10 μM. Cell viability is measured after 72 hours by MTS tetrazolium substrate and IC50 values are calculated.


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: BT474 breast cancer cells are implanted subcutaneously into Immune-deficient female mice (Nu/nu; age 8-12 weeks).
  • Formulation: 0.5% carboxymethylcellulose (CMC)
  • Dosages: 10, 30 or 100 mg/kg
  • Administration: Oral daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL warmed (90.56 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC
For best results, use promptly after mixing.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 386.47
Formula

C22H18N4OS

CAS No. 319460-85-0
Storage powder
in solvent
Synonyms AG 013736

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04033991 Not yet recruiting Drug: Sunitinib|Drug: Axitinib Carcinoma|Renal Cell Pfizer September 2019 --
NCT03472560 Active not recruiting Drug: Avelumab (MSB0010718C)|Drug: Axitinib (AG-013736) Non-Small Cell Lung Cancer|Urothelial Cancer Pfizer May 2 2018 Phase 2
NCT03592199 Active not recruiting Drug: Sunitinib Clear Cell Renal Cell Carcinoma Instituto do Cancer do Estado de São Paulo|Pfizer December 11 2017 Phase 2
NCT03289533 Active not recruiting Drug: Avelumab (MSB0010718C)|Drug: Axitinib (AG-013736) Carcinoma Hepatocellular Pfizer September 8 2017 Phase 1
NCT00460603 Completed Drug: bevacizumab|Drug: AG-013726|Drug: AG-013736 (axitinib) Colorectal Neoplasms Pfizer January 2006 Phase 1|Phase 2
NCT00219557 Completed Drug: Gemcitabine|Drug: AG-013736 Pancreatic Neoplasms Pfizer July 5 2005 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    We would like to store at -80℃ after it dissolved in CMC. Do you have any infomation about the suggested concentration in CMC?

  • Answer:

    Axitinib in 0.5% CMC at up to 30mg/ml is a suspension for oral gavage administration only. We don't suggest customer to freeze down the solution but to make fresh if possible. Customer can store it for 1-2 weeks at 4 degree for continuous use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID