CAS NO: | 1394820-69-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) withIC50s of 6.7, 1.9 and<1.0 nM forc-Met,VEGFR2andAxl, respectively. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | 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 IC50values of 8.6 and 6.3 nM, respectively[1]. | ||||||||||||||||
体内研究 (In Vivo) | 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[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 556.58 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C31H29FN4O5 | ||||||||||||||||
CAS 号 | 1394820-69-9 | ||||||||||||||||
中文名称 | 宁格替尼 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 16.67 mg/mL(29.95 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |