185049-54-1
Chemical Structure
A-176120
- CAS No.: 185049-54-1
- Formula:C33H29NO9
- Molecular Weight:583.58
IUPAC Name: 5-((2-ethoxybenzyl)(3-(p-tolyloxy)benzyl)carbamoyl)benzene-1,2,4-tricarboxylic acid
InChIKey: NHCMSBSXCWMLKE-UHFFFAOYSA-N
SMILES: O=C(C1=CC(C(N(CC2=CC=CC=C2OCC)CC3=CC=CC(OC4=CC=C(C)C=C4)=C3)=O)=C(C(O)=O)C=C1C(O)=O)O
Biological Activity: A-176120 is a selective inhibitor of farnesyl transferase (IC50=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC50=423 nM), GGTaseII (IC50=3000 nM), and SSase (IC50>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion[1].
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A-176120 | A-176120 is a selective inhibitor of farnesyl transferase (IC50=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC50=423 nM), GGTaseII (IC50=3000 nM), and SSase (IC50>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion. | |||||||||||||||||||||
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