Axitinib (AG 013736)

Licensed by Pfizer Catalog No.S1005

For research use only.

Axitinib (AG 013736) 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.

Axitinib (AG 013736) Chemical Structure

CAS No. 319460-85-0

Selleck's Axitinib (AG 013736) has been cited by 127 publications

Purity & Quality Control

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Biological Activity

Description Axitinib (AG 013736) 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)
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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 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LZRmlEPTB;MD6wNFAxPTF|IN88US=> M2q4fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
NCI-H1703 NITaOZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\yfXJKSzVyPUCuNFAxQTB{IN88US=> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
KASUMI-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3OSohKSzVyPUCuNFA3QDJizszN M{XVcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
CGTH-W-1 NVLxVnhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrWTWM2OD1yLkCwO|IzKM7:TR?= NEPIXmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
A204 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHwTWM2OD1yLkCwPVkzKM7:TR?= NFz4N4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
HOP-62 NGHJXWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwMUC4N|Yh|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
H-EMC-SS NFfJNmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXGfWM2UUN3ME2wMlEyODB3IN88US=> NXfEcVZqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
KU812 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD5TWM2OD1yLkG2OVc4KM7:TR?= Ml61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
EM-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwMU[4NVYh|ryP NWKxTY1YRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
LAMA-84 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[xTWM2OD1yLkG3OlY2KM7:TR?= NUHSUI0{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
JAR M3HR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrkTWM2OD1yLkKzPVg6KM7:TR?= NFnvU4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
G-361 MkDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfxcmNsUUN3ME2wMlMzOzJ3IN88US=> Mn;ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
KG-1 M4HZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwM{e2OFIh|ryP NF22ZZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
BV-173 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjhZW9KSzVyPUCuN|k{OiEQvF2= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
K5 M3TZcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwNEKxNlch|ryP MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
MEG-01 NYjPPItST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwNEKzOlEh|ryP NXrmVHE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
MFM-223 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXiXZdKSzVyPUCuOFQ4PzZizszN MnXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
BE-13 Mm\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvncZdKSzVyPUCuOVExODhizszN MljIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
NEC8 MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD1TWM2OD1yLkeyNVE{KM7:TR?= NWHYW2wzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
SW756 M3vRbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwOUm4OFYh|ryP MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
A2780 NULqRnRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTFwMEGxOFYh|ryP MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
NB14 MoTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFwMEG4NFEh|ryP M4j4SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
H4 NXX0dYRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7EfWxKSzVyPUGuNFY1OjJizszN MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
SK-OV-3 MmGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDwVWlKSzVyPUGuNFY3OzNizszN NGLsTWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
AN3-CA MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTFwMEizPFkh|ryP MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
A427 NVr4doJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXTTWM2OD1zLkGwN|gyKM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
ES7 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULsRXFuUUN3ME2xMlEyOzN2IN88US=> MkfqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
AGS NXLtbXFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zn[WlEPTB;MT6xNVM6PSEQvF2= NV\E[5B4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
G-402 M1v6d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjLcZdKUUN3ME2xMlE1Pjl2IN88US=> Ml3VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
ES5 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHlc2IxUUN3ME2xMlE4OjR6IN88US=> MorjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
DEL NYfhT|lDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTFwMkW0OVch|ryP MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
NB10 NVnxfXM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTFwM{K1OVch|ryP M{W1blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
NCI-H1581 MkPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jhUGlEPTB;MT6zPVA1OiEQvF2= Mk\6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
D-566MG NIe5TIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;1TWM2OD1zLkSwOlg{KM7:TR?= NEfTUZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
LXF-289 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TLV2lEPTB;MT60N|k6PiEQvF2= MoTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
BT-549 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzU[WVKSzVyPUGuOVY6ODlizszN NHyzbWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
NKM-1 M2PVT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTwVGtVUUN3ME2xMlYxPTV4IN88US=> MmnHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
SW780 NYPLdFVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGL0blNKSzVyPUGuOlUyPThizszN MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
NCI-H292 MkDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTFwNk[zPFMh|ryP NFz3eoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
HMV-II MkjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTFwN{C0PFgh|ryP M1rlbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
ALL-PO NIfVbmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjBTYd6UUN3ME2xMlgxODF3IN88US=> MoGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
UACC-257 Mne3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HlTWlEPTB;MT64NlE3OyEQvF2= M4fmd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
PA-1 NVLnW3BPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjIVW5KSzVyPUGuPFI4OjVizszN M331eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
HD-MY-Z M{LmbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvNN4dzUUN3ME2xMlg3OjhzIN88US=> NEf4SHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
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BHT-101 M3\we2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ftRmlEPTB;MkmuN|IyKM7:TR?= NUCzXnp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
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HUVEC MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVHmcpIyOSCqch?= NF\VO3VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JHZGT0Zvc4TpcZVt[XSnZDDIWXZGSyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHlicILlbY5kfWKjdHXkJIZweiBzIHjyJIZwdGyxd3XkJIJ6KGGmZHn0bY9vKG:oIG\FS2YhdWWjc4Xy[YQh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvODByNTFOwG0v Mn2wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQmNpTU2ETEyvZV4>
HUVEC MnzPRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MX[xJIhz NWO1TotYSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBXTUeILYP0bY12dGG2ZXSgTHVXTUNiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBnd2yub4fl[EBjgSCjZHTpeIlwdiCxZjDWSWdHKG2nYYP1doVlKGGodHXyJFczKGi{czDpckBxemW|ZX7j[UBw\iCjbHL1cYlvKGK7IF3UWEBie3OjeTygTWM2OCB;IECuNFAzPyEQvF2u MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+R4hGVUKOPD;hQi=>
A549 NGDnUpdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4HmfFQ5KGi{cx?= M33iW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgWmVITi2|dHnteYxifGWmIHj1cYFvKEF3NEmgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSB{Mj60JO69VS5? NVTtVWh6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRkOqRV3CUFww[T5?
HepG2 MmjRRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnfpOFghcHK| M3LQOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgWmVITi2|dHnteYxifGWmIHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxKD1iM{iuO{DPxE1w NVr0TYxERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRkOqRV3CUFww[T5?
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 ; PARP / cleaved PARP / caspase-3 / cleaved caspase-3 31205508
Immunofluorescence alpha-tubulin 26474283
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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]

  • Animal Models: BT474 breast cancer cells are implanted subcutaneously into Immune-deficient female mice (Nu/nu; age 8-12 weeks).
  • 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

* 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05172440 Active not recruiting Drug: tislelizumab combined with axitinib Neoadjuvant Therapy Hongqian Guo|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School December 9 2021 Phase 2
NCT04941768 Recruiting -- Carcinoma Renal Cell Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany|Merck Serono GmbH an affiliate of Merck KGaA Darmstadt Germany August 9 2021 --
NCT04682587 Active not recruiting Drug: Axitinib|Drug: Avelumab|Drug: Pembrolizumab Renal Cell Carcinoma Pfizer February 24 2021 --
NCT04669366 Completed Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer January 20 2021 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
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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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