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BMS-817378 Sale

(Synonyms: [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) 目录号 : GC17772

Potent ATP competitive inhibitor of Met/VEGFR2

BMS-817378 Chemical Structure

Cas No.:1174161-69-3

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5mg
¥882.00
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10mg
¥1,649.00
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50mg
¥4,988.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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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

Chemical Properties

Cas No. 1174161-69-3 SDF
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 SMILES ClC1=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°C
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1 mg 5 mg 10 mg
1 mM 1.7276 mL 8.6378 mL 17.2756 mL
5 mM 0.3455 mL 1.7276 mL 3.4551 mL
10 mM 0.1728 mL 0.8638 mL 1.7276 mL
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