Ningetinib 是一种有效的口服生物可用的小分子酪氨酸激酶抑制剂 (TKI)，对 c-Met，VEGFR2 和 Axl 的 IC₅₀ 值分别为 6.7, 1.9 和 <1.0 nM。

Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC 50 s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

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VEGFR2 1.9 nM (IC50)

Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. In cell-based functional assays, Ningetinib (CT053PTSA) inhibits HGF and VEGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 8.6 and 6.3 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib (CT053PTSA) potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. In orthotopic U87MG human glioblastoma xenograft model, Ningetinib prolongs the median survival time (MST) and yields significant increase in life-span value (ILS=32%, p=0.003) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Ning Xi, et al. Abstract 1755: CT053PTSA, a novel c-MET and VEGFR2 inhibitor, potently suppresses angiogenesis and tumor growth. Cancer Res 2014;74(19 Suppl):Abstract nr 1755.

In Vitro: DMSO : 16.67 mg/mL (29.95 mM; Need ultrasonic)配制储备液