Ningetinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ningetinib (CT053PTSA) 是一种口服生物可利用的酪氨酸激酶抑制剂，对于 Axl、VEGFR2 和 c-Met 的 IC50 值分别<1.0、1.9 和 6.7 nM。

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.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.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.

——

——

CT-053,CT053PTSA

Angiogenesis

c-Met/HGFR

c-Met| VEGFR2| AXL

Cancer

Non-small cell lung Cancer; Renal Cancer

1394820-69-9

556.58

C31H29FN4O5

>98% (HPLC)

DMSO:15 mg/mL (26.95 mM; Need ultrasonic)

Cc1c(C(=O)Nc2ccc(Oc3ccnc4cc(OCC(C)(C)O)ccc34)c(F)c2)c(=O)n(-c2ccccc2)n1C

——

(-20℃)

With Ice Pack

≥ 2 years