CAS NO: | 319460-85-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | Axitinib is a multi-targeted tyrosine kinase inhibitor withIC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM forVEGFR1,VEGFR2,VEGFR3andPDGFRβ, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Axitinib (AG-013736) is a potent and selective inhibitor of VEGFR 1 to 3. In transfected or endogenous RTK-expressing cells, Axitinib potently blocks growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 with average IC50values of 0.2 and 0.1 to 0.3 nM, respectively. Cellular activity against VEGFR-1 is 1.2 nM (measured in the presence of 2.3% bovine serum albumin), equivalent to an absolute IC50of ~0.1 nM, based on protein binding of Axitinib. The potency against murine VEGFR-2 (Flk-1) in Flk-1-transfected NIH-3T3 cells is 0.18 nM, similar to that of its human homologue. Axitinib shows ~8- to 25-fold higher IC50against the closely related type III and V family RTKs, including PDGFR-β (1.6 nM), KIT (1.7 nM), and PDGFR-α (5 nM); nanomolar concentrations of Axitinib blocks PDGF BB-mediated human glioma U87MG cell (PDGFR-β-positive) migration but not proliferation[2]. | ||||||||||||||||
体内研究 (In Vivo) | A single oral dose of Axitinib (100 mg/kg) markedly suppresses murine VEGFR-2 phosphorylation for up to 7 h compared with control tumors. Axitinib rapidly inhibits VEGF-induced vascular permeability in the skin of mice; the inhibition is dose-dependent and directly correlated with drug concentration in mice. Pharmacokinetic/pharmacodynamic analysis indicate an unbound EC50of 0.46 nM. Similar inhibitory effects are also shown in the skin of MV522 tumor-bearing mice without exogenous VEGF-A stimulation. Axitinib inhibits the growth of human xenograft tumors in mice. Axitinib produces dose-dependent growth delay regardless of initial tumor size, model type, or implant site[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 386.47 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H18N4OS | ||||||||||||||||
CAS 号 | 319460-85-0 | ||||||||||||||||
中文名称 | 阿昔替尼;阿西替尼 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 20.83 mg/mL(53.90 mM;Need ultrasonic) 配制储备液
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