| 货号 | 12961S |
| 使用方法 | Axitinib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.29 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 1-1000 nM for 0.5-2 hr prior to treating with a stimulator. It can also be used alone, with varying treatment times lasting up to 72 hr. |
| 供应商 | CST |
| 背景 | Axitinib is a selective inhibitor of VEGFR, PDGFR, and c-kit tyrosine kinases. Researchers performing cellular phosphorylation assays have shown that axitinib very potently inhibits VEGF-1, -2, and -3 with IC50 values of approximately 1.2 nM, 0.2 nM, and 0.1-0.3 nM, respectively. It also effectively inhibits PDGF-α (IC50 = 5.0 nM), PDGF-β (IC50 = 1.6 nM), and c-kit (IC50 = 1.7 nM) (1). Axitinib exhibits little activity against a variety of off-target protein kinases when used at 1 µM (1). It inhibits VEGF-induced endothelial cell proliferation, survival, and tube formation, as well as phosphorylation of downstream targets Akt, eNOS, and ERK1/2 in a dose-dependent manner (1). Research studies demonstrate that axitinib suppresses T cell proliferation in a dose dependent manner through G2/M mitotic arrest, while apoptosis is largely prevented though stabilization of Mcl-1 and inactivation of caspase-9 (2). Axitinib has been shown to reduce both hypoxic-induced tissue permeability and overexpression/secretion of VEGF and PDGF in HUVE and RPE cells, as well as alter junction protein expression (3). |
| 存放说明 | -20C |
| 纯度 | >99% |
| 计算分子量 | 386.47 g/mol |
| 参考文献 | 1 . Hu-Lowe, D.D. et al. (2008) Clin Cancer Res 14, 7272-83. 2 . Stehle, F. et al. (2013) J Biol Chem 288, 16334-47. 3 . Kernt, M. et al. (2012) Growth Factors 30, 49-61. |
Chemical structure of axitinib. | |
Western blot analysis of extracts from NIH/3T3 cells, serum-starved overnight and untreated (-) or pretreated with Axitinib (100 nM, 2 hr; +) prior to treatment with Human Platelet-Derived Growth Factor BB (hPDGF-BB) #8912 (100 ng/ml, 5 min; +), using Phospho-PDGF Receptor β (Tyr1009) (42F9) Rabbit mAb #3124 (upper) or PDGF Receptor β (28E1) Rabbit mAb #3169 (lower). | |
Western blot analysis of extracts from NCI-H526 cells, serum-starved overnight and untreated (-) or pretreated with Axitinib (1000 nM, 2 hr; +) prior to treatment with Human Stem Cell Factor (hSCF) #8925 (100 ng/ml, 5 min; +), using Phospho-c-Kit (Tyr703) (D12E12) Rabbit mAb #3073 (upper) or c-Kit (D13A2) XP® Rabbit mAb #3074 (lower). |
