Axitinib (AG 013736)

For research use only. Not for use in humans.

Pfizer辉瑞授权 目录号:S1005 中文名称:阿西替尼

Axitinib (AG 013736) Chemical Structure

CAS No. 319460-85-0

Axitinib (AG 013736)是一种多靶点抑制剂,作用于 VEGFR1VEGFR2VEGFR3,PDGFRβ和c-Kit,在猪主动脉内皮细胞中IC50分别为0.1 nM,0.2 nM,0.1-0.3 nM,1.6 nM和1.7 nM。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 647.01 现货
RMB 570.91 现货
RMB 975.25 现货
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客户使用Selleck生产的Axitinib (AG 013736)发表文献115篇:

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述 Axitinib (AG 013736)是一种多靶点抑制剂,作用于 VEGFR1VEGFR2VEGFR3,PDGFRβ和c-Kit,在猪主动脉内皮细胞中IC50分别为0.1 nM,0.2 nM,0.1-0.3 nM,1.6 nM和1.7 nM。
特性 Axitinib与目前使用的sorafenib相比,作为二代治疗法,更有效。
靶点
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
体外研究

Axitinib是受体激酶抑制剂,作用于VEGFR-1, VEGFR-2,VEGFR-3, PDGFR-β和c-KIT时IC50分别为0.1 , 0.2, 0.1-0.3, 1.6 和1.7 nM 。[1]Axitinib可以阻断VEGFR的自磷酸化作用,VEGF调节的内皮细胞活力,微管形成,及下游信号。Axitinib抑制多种细胞系的增殖,如作用于IGR-N91, IGR-NB8, SH-SY5Y ,无VEGF刺激的HUVEC时IC50分别为>1000 nM, 849 nM, 274 nM和573 nM。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell MkjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DtXmlEPTB;MD6wNFAxPTF|IN88US=> MlXTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
NCI-H1703 MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwMECwPVAzKM7:TR?= NHnxdpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
KASUMI-1 NUTDRWdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV6yS5RWUUN3ME2wMlAxPjh{IN88US=> NGPUWFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
CGTH-W-1 Ml[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwMEC3NlIh|ryP Mmf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
A204 NXf6ZWU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml35TWM2OD1yLkCwPVkzKM7:TR?= M4jnN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
HOP-62 M3nh[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwMUC4N|Yh|ryP M1TQNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
H-EMC-SS NVfWeYdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq4THM4UUN3ME2wMlEyODB3IN88US=> NHr1V5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
KU812 MlTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHldndVUUN3ME2wMlE3PTd5IN88US=> NH\zblM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
EM-2 NYf3d4s1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\zTWM2OD1yLkG2PFE3KM7:TR?= M{[1VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
LAMA-84 NGX2eJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7qPZFHUUN3ME2wMlE4PjZ3IN88US=> M{OyblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
JAR NGT1eo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nkXWlEPTB;MD6yN|k5QSEQvF2= NFjRdFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
G-361 MkTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37FTWlEPTB;MD6zNlMzPSEQvF2= Mn61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
KG-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwM{e2OFIh|ryP M{HO[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
BV-173 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfHN3EyUUN3ME2wMlM6OzJizszN NGHsTJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
K5 NWrMO|YyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkH4TWM2OD1yLkSyNVI4KM7:TR?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
MEG-01 NH64OHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XOZWlEPTB;MD60NlM3OSEQvF2= NWDtWJN{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
MFM-223 M3HBd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTrVJBzUUN3ME2wMlQ1Pzd4IN88US=> NWf0eZg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
BE-13 NG\DWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7MOohSUUN3ME2wMlUyODB6IN88US=> M1HpRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
NEC8 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\jV4RKSzVyPUCuO|IyOTNizszN M4\TNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
SW756 M1XuVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPIcWpJUUN3ME2wMlk6QDR4IN88US=> NH3vNFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
A2780 MmjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTFwMEGxOFYh|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
NB14 Ml3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvhTWM2OD1zLkCxPFAyKM7:TR?= M2PSU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
H4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TjbWlEPTB;MT6wOlQzOiEQvF2= NXnqdGo5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
SK-OV-3 NE[4RVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P0TWlEPTB;MT6wOlY{OyEQvF2= MmPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
AN3-CA NYr2Smo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTFwMEizPFkh|ryP M3zlWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
A427 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHQTWM2OD1zLkGwN|gyKM7:TR?= NEe2RWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
ES7 MljnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NViwcIpCUUN3ME2xMlEyOzN2IN88US=> NUGzUYN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
AGS NI\wcFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwMUGzPVUh|ryP M{LiUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
G-402 NF31V2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXhTWM2OD1zLkG0Olk1KM7:TR?= M4XacVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
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DEL MkDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX34eIpOUUN3ME2xMlI2PDV5IN88US=> M4HRfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
NB10 NUTDWJhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrZTWM2OD1zLkOyOVU4KM7:TR?= M{P2O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
NCI-H1581 MoXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLadnVxUUN3ME2xMlM6ODR{IN88US=> M2nwS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
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BT-549 NH70XXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rjVGlEPTB;MT61OlkxQSEQvF2= Mly3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
NKM-1 NYnHbGJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4G3Z2lEPTB;MT62NFU2PiEQvF2= MmTUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
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NB-EBc1 MX3xTHRUKGG|c3H5 NHXabGVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NIHXVlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 NULkWVk1eUiWUzDhd5NigQ>? Mo\TdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
HUVEC MoGxRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NYjoSpUyOSCqch?= M4r6emFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgWmVITi2|dHnteYxifGWmIFjVWmVEKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCycnXpcoN2[mG2ZXSg[o9zKDFiaIKg[o9tdG:5ZXSgZpkh[WSmaYTpc44hd2ZiVlXHSkBu\WG|dYLl[EBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4xODB3IN88UU4> M37BXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5EcEWPQly8M4E,
HUVEC NIH1Vm1CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MlLYNUBpeg>? M2GzW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgWmVITi2|dHnteYxifGWmIFjVWmVEKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCycnXpcoN2[mG2ZXSg[o9zKDFiaIKg[o9tdG:5ZXSgZpkh[WSmaYTpc44hd2ZiVlXHSkBu\WG|dYLl[EBi\nSncjC3NkBpenNiaX6gdJJme2WwY3Wgc4Yh[WykdX3pckBjgSCPVGSgZZN{[XluIFnDOVAhRSByLkCwNlch|ryPLh?= NYe3fVNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRkOqRV3CUFww[T5?
A549 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1jtbFQ5KGi{cx?= NWjBZ453SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBXTUeILYP0bY12dGG2ZXSgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB2ODDodpMh[nliQ1PLPEBie3OjeTygTWM2OCB;IEKyMlQh|ryPLh?= Ml7nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQmNpTU2ETEyvZV4>
HepG2 M{jjdmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MWe0PEBpenN? NHTie4lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JHZGT0Zvc4TpcZVt[XSnZDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB2ODDodpMh[nliQ1PLPEBie3OjeTygTWM2OCB;IEO4Mlch|ryPLh?= MVq8ZUB1[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
体内研究 Axitinib抑制常位移植模型,如M24met (黑色素瘤), HCT-116 (结肠直肠癌), 和SN12C (肾细胞癌)。[1]活体研究显示,按动物体重,每千克口服处理30mg Axitinib,与没有Axitinib处理的对照组相比,实验组推迟肿瘤生长达到11.4天;且用于IGR-N91侧腹移植瘤时,与对照组(密度为49)相比实验组(密度降为21)降低血管密度。[2]Axitinib在多种肿瘤包括肾细胞癌,甲状腺癌,非小细胞肺癌,黑色素瘤中显示出单一药效活性。

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

细胞受体激酶磷酸化实验:

生成过量表达全长VEGFR-2, PDGFR-β, 和KIT的PAE 细胞,及过量表达鼠VEGFR-2 (Flk-1) 或 PDGFR-α的NIH-3T3细胞。用2.5 µg/mL VEGFR-2抗体, 0.75 µg/mL anti-PDGFR-β 抗体, 0.25 µg/mL anti-PDGFR-α 抗体, 及0.5 µg/mL anti-KIT 抗体包被96孔板,每孔100ul。或者用1.20 µg/mL Flk-1抗体制成酶联免疫吸附(ELISA)捕获板。通过ELISA测定RTK的磷酸化作用。
细胞实验:[2]
- 合并
  • Cell lines: HUVEC,SH-SY5Y, IGR-N91,和IGR-NB8细胞
  • Concentrations: 1 nM 到10 µM
  • Incubation Time: 72小时
  • Method: HUVEC, SH-SY5Y, IGR-N91和IGR-NB8细胞系按5x104密度接种在96孔板上,培养24小时。加入浓度不等(1 nM到10 µM)的Axitinib。72小时后,通过 MTS四唑基底物测定细胞活力,计算IC50值。
    (Only for Reference)
动物实验:[3]
- 合并
  • Animal Models: BT474胸腺癌细胞皮下移植到雌性免疫缺陷小鼠内(Nu/nu;8-12周大)
  • Dosages: 10, 30或100 mg/kg
  • Administration: 每天口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 35 mg/mL warmed (90.56 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 386.47
化学式

C22H18N4OS

CAS号 319460-85-0
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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 Recruiting Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer January 20 2021 --
NCT04626128 Recruiting Drug: CLS-AX|Drug: Anti-VEGF Neovascular Age-related Macular Degeneration Clearside Biomedical Inc. December 15 2020 Phase 1|Phase 2
NCT04637204 Completed Drug: Cabozantinib|Drug: Axitinib Renal Cell Carcinoma Ipsen November 24 2020 --

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

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

  • 回答:

    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.

VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

相关VEGFR产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID