WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205574
Description: PCI-27483 is a reversible small-molecule inhibitor of activated factor VII (factor VIIa) with potential antineoplastic and antithrombotic activities. FVII, a serine protease, becomes activated (FVIIa) upon binding with TF forming the FVIIa/TF complex, which induces intracellular signaling pathways by activating protease activated receptor 2 (PAR-2). Upon subcutaneous administration, factor VIIa inhibitor PCI-27483 selectively inhibits factor FVIIa in the VIIa/TF complex, which may prevent PAR-2 activation and PAR2-mediated signal transduction pathways, thereby inhibiting tumor cell proliferation, angiogenesis, and metastasis of TF-overexpressing tumor cells.
MedKoo Cat#: 205574
Chemical Formula: C26H24N6O9S
Exact Mass: 596.13255
Molecular Weight: 596.56856
Elemental Analysis: C, 52.35; H, 4.05; N, 14.09; O, 24.14; S, 5.37
Synonym: PCI27483; PCI-27483; PCI 27483.
IUPAC/Chemical Name: (S)-2-(2-(5-(5-carbamimidoyl-1H-benzo[d]imidazol-2-yl)-2',6-dihydroxy-5'-sulfamoyl-[1,1'-biphenyl]-3-yl)acetamido)succinic acid.
InChi Key: WDJHHCAKBRKCLW-IBGZPJMESA-N
InChi Code: InChI=1S/C26H24N6O9S/c27-24(28)12-1-3-17-18(8-12)32-25(31-17)16-6-11(7-21(34)30-19(26(38)39)10-22(35)36)5-15(23(16)37)14-9-13(42(29,40)41)2-4-20(14)33/h1-6,8-9,19,33,37H,7,10H2,(H3,27,28)(H,30,34)(H,31,32)(H,35,36)(H,38,39)(H2,29,40,41)/t19-/m0/s1
SMILES Code: O=S(C1=CC=C(O)C(C2=C(O)C(C3=NC4=CC(C(N)=N)=CC=C4N3)=CC(CC(N[C@H](C(O)=O)CC(O)=O)=O)=C2)=C1)(N)=O
Pharmacyclics’s Factor VIIa inhibitor PCI-27483 is a novel first-in-human small molecule inhibitor that selectively targets FVIIa. As an inhibitor of FVIIa, PCI-27483 has two potential mechanisms of action: 1) inhibition of intracellular signaling involved in tumor growth and metastases and 2) inhibition of early coagulation processes associated with thromboembolism.
1. Manufacture, compositions and uses of coagulation factor VIIa modulator, By Loury, David; Purro, Norbert, From PCT Int. Appl. (2009), WO 2009052323 A2 20090423.