英国Kinasechem现货XL-184freebase (Cabozantinib) CAS No. 849217-68-1

保质期 ：2年

供应商 ：Kinasechem

英文名 ：XL-184

CAS号 ：849217-68-1

保存条件 ：-20℃

规格 ：1ML/2mg/5mg/10mg

MW：501.51
溶解性：DSMO 117 mg/mL Water <1 mg/ml Ethanol <1 mg/ml
纯度：>99%
描述：
1. Cabozantinib inhibits endothelial cell tubule formation in vitro Cabozantinib inhibited tubule formation with an IC 50 value of 6.7 nmol/L. Cabozantinib also inhibited tubule formation in response to conditioned media derived from cultures of MDA-MB-231 (IC 50 =5.1 nmol/L), A431 (IC 50= 4.1 nmol/L), HT1080 (IC 50 = 7.7 nmol/L), and B16F10 (IC 50 = 4.7 nmol/L) cells.
2. Cabozantinib inhibits cellular migration and invasion Cabozantinib potently inhibited HGF-induced migration (IC 50 = 31 nmol/L) and invasion (IC 50 = 9 nmol/L) of B16F10 cells. VEGF- and HGF-mediated migration of proangiogenic murine MS1 endothelial cells were also sensitive to cabozantinib with IC 50 values of 5.8 and 41 nmol/L. Cabozantinib inhibits MET and VEGFR2 phosphorylation in vivo. A single 100 mg/kg oral dose of cabozantinib resulted in inhibition of phosphorylation of MET 2 to 8 hours postdose in H441 tumors that harbor constitutively phosphorylated MET.
参考文献：
[1] Zhang, Y., F. Guessous, et al. (2010). "XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC." IDrugs 13(2): 112-121.
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