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VX-680

品牌
Sigma-Aldrich
CAS
639089-54-6
货号
SML2158
包装型号
规格纯度
≥98% (HPLC)
参考价格
801.71 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

生化/生理作用

VX-680 is an ATP site-targeting potent aurora kinase inhibitor (Aurara A/B/C Ki(app) = 0.6/18/4.6 nM) that affects FLT3, BCR-Abl, BCR-Abl (T315I), Lck, ITK, Src, and Fyn only at higher concentrations (Ki(app) = 30, 30, 42, 80, 220, 350, 520 nM, respectively) and exhibits little inhibitory potency toward 52 other kinases (Ki(app) >1 μM). VX-680 exhibits potent antiproliferation activity in a wide variety of cancer cultures (IC50 from 15 to 113 nM) as a result of cell cycle arrest and apoptosis induction, as well as causes tumor retardation (by 98% on day 13; 75 mg/kg b.i.d i.p.; HL-60 in mice) and regression (2 mg/kg/h 3 d/wk i.v. infusion; HCT116 in rats) in vivo. Crystallography data reveal a tight association of VX-680 with a hydrophobic pocket present only in a closed, inactive kinase conformation, which forms the basis of its selectivity profile, including its activity toward wild-type and the Imatinib-resistant (T315I) Abl.

基本信息

经验(实验)分子式C23H28N8OS
分子量464.59
MDL编号MFCD13185152
NACRESNA.77

产品性质

测定≥98% (HPLC)
形式powder
颜色 white to beige
溶解性DMSO: 2 mg/mL, clear
储存温度2-8℃
SMILES stringO=C(C1CC1)NC(C=C2)=CC=C2SC3=NC(N4CCN(C)CC4)=CC(NC5=NNC(C)=C5)=N3

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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