Ningetinib
产品名称:Ningetinib
产品描述:
产品描述 | Ningetinib (CT053PTSA) is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively. |
靶点活性 | Axl:<1 nM (cell free), c-Met:6.7 nM (cell free), VEGFR2:1.9 nM (cell free) |
体外活性 | In cell-based functional assays, Ningetinib inhibits VEGF and HGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 6.3 and 8.6 nM, respectively. |
体内活性 | In the orthotopic U87MG human glioblastoma xenograft model, Ningetinib prolongs the median survival time and yields a significant increase in life-span value (ILS=32%) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group. When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. |
别名 | CT053PTSA, CT-053, 宁格替尼 |
分子量 | 556.58 |
分子式 | C31H29FN4O5 |
CAS No. | 1394820-69-9 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 15 mg/mL (26.95 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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