Axitinib (AG 013736)

For research use only.

Licensed by Pfizer Catalog No.S1005

112 publications

Axitinib (AG 013736) Chemical Structure

CAS No. 319460-85-0

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) GBP 64 In stock
GBP 57 In stock
GBP 98 In stock
GBP 177 In stock
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Selleck's Axitinib (AG 013736) has been cited by 112 publications

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Choose Selective VEGFR Inhibitors

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)
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 NHrKdHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXySlZKSzVyPUCuNFAxODVzMzFOwG0> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
NCI-H1703 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\DVWlEPTB;MD6wNFA6ODJizszN NYfzdZFQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
KASUMI-1 NIDVZ5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvQTWM2OD1yLkCwOlgzKM7:TR?= MmLsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
CGTH-W-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jiOmlEPTB;MD6wNFczOiEQvF2= M1i5ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
A204 NIC1S4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nZdmlEPTB;MD6wNFk6OiEQvF2= M1W1WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
HOP-62 NH3XO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwMUC4N|Yh|ryP MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
H-EMC-SS MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrRTWM2OD1yLkGxNFA2KM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
KU812 NWTOSGxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXtTWM2OD1yLkG2OVc4KM7:TR?= M3vJUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
EM-2 NVrVTWhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljOTWM2OD1yLkG2PFE3KM7:TR?= NWjq[ZhsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
LAMA-84 NV74bIRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XmZWlEPTB;MD6xO|Y3PSEQvF2= NFL0UJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
JAR Mn7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwMkO5PFkh|ryP M1ywfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
G-361 M{iwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGOx[INKSzVyPUCuN|I{OjVizszN MlzBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
KG-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu2TWM2OD1yLkO3OlQzKM7:TR?= NELXbVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
BV-173 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUCxS|JpUUN3ME2wMlM6OzJizszN M3fZU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
K5 M1nSXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjZTWhDUUN3ME2wMlQzOTJ5IN88US=> M3r5[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
MEG-01 NE\FcJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLhRXNKSzVyPUCuOFI{PjFizszN NHz1So09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
MFM-223 M2C0Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37jTWlEPTB;MD60OFc4PiEQvF2= M{f5WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
BE-13 MlG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwNUGwNFgh|ryP NIjpVlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
NEC8 MoLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnXWoQ1UUN3ME2wMlczOTF|IN88US=> MkW5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
SW756 NEnwPZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHvTWM2OD1yLkm5PFQ3KM7:TR?= NX;jUJJIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
A2780 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVqzdIhiUUN3ME2xMlAyOTR4IN88US=> NWXLVVZkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
NB14 MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfyTWM2OD1zLkCxPFAyKM7:TR?= NWexeVdrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
H4 M1XCc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFwME[0NlIh|ryP M4fSUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
SK-OV-3 MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LxT2lEPTB;MT6wOlY{OyEQvF2= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
AN3-CA MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvyTINKSzVyPUGuNFg{QDlizszN MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
A427 M{Xzc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XUb2lEPTB;MT6xNFM5OSEQvF2= NWjoOYhERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
ES7 M{fob2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzqTHk3UUN3ME2xMlEyOzN2IN88US=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
AGS M4Lpd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFwMUGzPVUh|ryP MlS4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
G-402 NWHDWHR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPUU|lKSzVyPUGuNVQ3QTRizszN NXrpUmxXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
ES5 NVv4Vm1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXnWIxKUUN3ME2xMlE4OjR6IN88US=> MkTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
DEL M37nc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojyTWM2OD1zLkK1OFU4KM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
NB10 NVfsbmxoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDCTWM2OD1zLkOyOVU4KM7:TR?= M{TEbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
NCI-H1581 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPGXYZbUUN3ME2xMlM6ODR{IN88US=> M130SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
D-566MG MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPWO5dKSzVyPUGuOFA3QDNizszN MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
LXF-289 NXzrO5lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDuTWM2OD1zLkSzPVk3KM7:TR?= M3O2cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
BT-549 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17ZZ2lEPTB;MT61OlkxQSEQvF2= NX;ZNIR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
NKM-1 NUXUVI51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTFwNkC1OVYh|ryP MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
SW780 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTKR3NKSzVyPUGuOlUyPThizszN NIjlVIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
NCI-H292 NFHhOI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXxT5JKSzVyPUGuOlY{QDNizszN M4W4WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
HMV-II M2LCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfrfXVKSzVyPUGuO|A1QDhizszN MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
ALL-PO MoPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFwOECwNVUh|ryP MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
UACC-257 M4HPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnKyTWM2OD1zLkiyNVY{KM7:TR?= M2jDb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
PA-1 M4j6bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLNO5FKSzVyPUGuPFI4OjVizszN NGHmbJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
HD-MY-Z MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwOE[yPFEh|ryP MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
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HUVEC NHfPVlFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1LnTVEhcHJ? MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IG\FS2Yue3SrbYXsZZRm\CCKVW\FR{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkheHKnaX7jeYJifGWmIH\vdkAyKGi{IH\vcIxwf2WmIHL5JIFl\Gm2aX;uJI9nKF[HR1[gcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNFAxPSEQvF2u Mkj4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQmNpTU2ETEyvZV4>
HUVEC MYPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MkixNUBpeg>? MlnrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDWSWdHNXO2aX31cIF1\WRiSGXWSWMh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KHC{ZXnuZ5Vj[XSnZDDmc5IhOSCqcjDmc4xtd3enZDDifUBi\GSrdHnvckBw\iCYRVfGJI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCrbjDwdoV{\W6lZTDv[kBidGK3bXnuJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwMECyO{DPxE1w MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+R4hGVUKOPD;hQi=>
A549 M1u2emFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NWD0S3ZjPDhiaILz NXX6RVIySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBXTUeILYP0bY12dGG2ZXSgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB2ODDodpMh[nliQ1PLPEBie3OjeTygTWM2OCB;IEKyMlQh|ryPLh?= NY\tc21IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRkOqRV3CUFww[T5?
HepG2 MX7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVW0PEBpenN? NX7MfGZOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBXTUeILYP0bY12dGG2ZXSgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPDT|gh[XO|YYmsJGlEPTBiPTCzPE44KM7:TT6= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+R4hGVUKOPD;hQi=>

... 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).
  • 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 powder
in solvent
Synonyms N/A
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)
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Step 2: Enter the in vivo formulation ()
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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)

  • Mass
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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 SDS / 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 SDS / 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):
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    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
NCT04682587 Active not recruiting Drug: Axitinib|Drug: Avelumab|Drug: Pembrolizumab Renal Cell Carcinoma Pfizer February 24 2021 --
NCT04637204 Completed Drug: Cabozantinib|Drug: Axitinib Renal Cell Carcinoma Ipsen November 24 2020 --
NCT04555603 Active not recruiting Drug: Inlyta|Drug: Bavencio|Drug: Keytruda Renal Cell Carcinoma Pfizer September 15 2020 --
NCT04522323 Active not recruiting Biological: MEDI5752|Drug: Axitinib Advanced Renal Cell Carcinoma MedImmune LLC August 5 2020 Phase 1
NCT04459663 Not yet recruiting Drug: Toripalimab injection combine with Axitinib Non-small Cell Lung Cancer Li Zhang MD|Sun Yat-sen University August 31 2020 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