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Ningetinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ningetinib图片
CAS NO:1394820-69-9
包装与价格:
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

产品名称
宁格替尼
产品介绍
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-MetVEGFR2AxlIC50值分别为 6.7, 1.9 和<1.0 nM。
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

VEGFR2

1.9 nM (IC50)

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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL(29.95 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7967 mL8.9834 mL17.9669 mL
5 mM0.3593 mL1.7967 mL3.5934 mL
10 mM0.1797 mL0.8983 mL1.7967 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。