| 保质期 | 2年 |
| 保存条件 | - 20℃ |
| 英文名 | XL-184(Cabozantinib)（Targets：VEGFR2，c-Met，c-Kit，Tie2，FLT-3） |
| CAS号 | 849217-68-1 |
| 供应商 | 上海高创 |
| 规格 | 2mg |
| SKU:K1008 | M. Wt:501.51 | ||
| Formula:C28H24FN3O5 | Solubility:DSMO 117 mg/mL Water <1 mg/ml Ethanol <1 mg/ml | ||
| Purity:>99% | Storage:2 years at -20 degrees centigrade | ||
| CAS No.:849217-68-1 | |||
| Chemical NameN-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | |||
| Description | As a pan-tyrosine kinase inhibitor, XL-184 (BMS-907351, Cabozantinib) can potently inhibit VEGFR2, Met, Kit, Tie2 and FLT-3 with IC50 of 0.035 nM, 1.8 nM, 4.6 nM, 14.3 nM and 14.4 nM. | |||||
|---|---|---|---|---|---|---|
| Targets | VEGFR2 | c-Met | c-Kit | Tie2 | FLT-3 | |
| IC50 | 0.035 nM | 1.8 nM | 4.6 nM | 14.3 nM | 14.4 nM | |
| In vitro | 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. | |||||
| IN vivo | 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. | |||||
