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BMS-817378
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。
BMS-817378图片
CAS NO:1174161-69-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Potent ATP competitive inhibitor of Met/VEGFR2
Cas No.1174161-69-3
别名[3-[[4-((2-氨基-3-氯吡啶-4-基)氧基)-3-氟苯基]氨基甲酰基]-5-(4-氟苯基)-4-氧代-4H-吡啶-1-基]甲基磷酸二氢酯
化学名(Z)-N-(4-((3-chloro-2-imino-1,2-dihydropyridin-4-yl)oxy)-3-fluorophenyl)-5-(4-fluorophenyl)-4-oxo-1-((phosphonooxy)methyl)-1,4-dihydropyridine-3-carbimidic acid
Canonical SMILESClC1=C(OC2=C(F)C=C(/N=C(O)/C3=CN(COP(O)(O)=O)C=C(C3=O)C4=CC=C(F)C=C4)C=C2)C=CNC1=N
分子式C24H18ClF2N4O7P
分子量578.85
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Description:

IC50: 1.7 nM/15 nM for Met/VEGFR2

The signaling pathway of the receptor tyrosine kinase MET and its ligand hepatocyte growth factor is important for cell growth, survival, and motility and is functionally linked to the signaling pathway of VEGF, which is widely recognized as a key effector in angiogenesis and cancer progression. BMS-817378 is a potent ATP competitive inhibitor of Met/VEGFR2.

In vitro: BMS-794833, which is the active moiety of BMS-817378, is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of<3 nM. BMS-794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM [1].

In vivo: BMS-798433 shows greater than 50% TGI for at least one tumor doubling time with no toxicity observed during 14 days in GTL-16 human gastric tumor xenografts model. BMS-798433 also shows complete tumor stasis at 25 mg/kg against U87 glioblastoma model [1].

Clinical trial: BMS-817378 is now in its ascending multiple-dose study in subjects with advanced cancers.

Reference:
[1]http://worldwide. espacenet.com/publicationDetails/biblio?DB=EPODOC&II=0&adjacent=true&locale=en_EP&FT=D&date=20090730&CC=WO&NR=2009094417A1&KC=A1