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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Farnesyl transferase (FTase)-A-176120
A-176120

Chemical Structure : A-176120

CAS No.: 185049-54-1

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A-176120 (A176120)

货号: PC-23307Not For Human Use, Lab Use Only.

A-176120 is a potent, selective inhibitor of farnesyltransferase (FTase) with IC50 of 1.2 nM, inhibits Ras processing in H-ras-transformed NIH3T3 cells and HCT116 K-ras-mutated cells (ED50=1.6 and 0.5 uM, respectively).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

A-176120 is a potent, selective inhibitor of farnesyltransferase (FTase) with IC50 of 1.2 nM, inhibits Ras processing in H-ras-transformed NIH3T3 cells and HCT116 K-ras-mutated cells (ED50=1.6 and 0.5 uM, respectively).
A-176120 shows high selectivity over closely related enzymes geranylgeranyltransferase I (GGTaseI) (IC(50) 423+/-1.8 nM), geranylgeranyltransferase II (GGTaseII) (IC(50) 3000 nM) and squalene synthase (SSase) (IC(50)>10000 nM).
A-176120 exhibits anti-angiogenic potential by a decrease in Ras processing, cell proliferation and capillary structure formation of human umbilical vein endothelial cells (HUVEC), and a decrease in the secretion of vascular endothelial growth factor (VEGF) from HCT116 cells.
A-176120 reduced H-ras NIH3T3 tumour growth and extended the lifespan of nude mice inoculated with H- or K-ras-transformed NIH3T3 cells in vivo.

物理化学性质&存储条件

分子量 583.59
分子式 C33H29NO9
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-[[[(2-Ethoxyphenyl)methyl][[3-(4-methylphenoxy)phenyl]methyl]amino]carbonyl]-1,2,4-benzenetricarboxylic acid

参考文献

1. Tahir SK, et al. Eur J Cancer. 2000 Jun;36(9):1161-70.

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