Chemical Structure : A-176120
CAS No.:
185049-54-1
A-176120
(A176120)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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583.59
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Formula
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C33H29NO9
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-[[[(2-Ethoxyphenyl)methyl][[3-(4-methylphenoxy)phenyl]methyl]amino]carbonyl]-1,2,4-benzenetricarboxylic acid
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References
1. Tahir SK, et al. Eur J Cancer. 2000 Jun;36(9):1161-70.
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