PCI-27483

Research use only, not for human use.

PCI 27483 is an activated coagulation factor VIIa inhibitor with antithrombotic effects in a baboon model of arterial thrombosis.

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.

PCI-27483 inhibits the TF:FVIIa-complex induced phosphorylation of ERK1/2 and subsequent induction of c-fos in BxPC3 cells, a human pancreatic adenocarcinoma line that highly expresses TF. Furthermore, PCI-27483 blocks the TF:FVIIa induced secretion of IL8 in both BxPC3 cells and MDA-MB-231 breast cancer cells.

PCI-27483 shows dose-dependent inhibition of thrombus formation, fibrin accumulation and PT. PCI-27483 (4 mg/kg) shows comparable anticoagulation effects as 2 mg/kg enoxaparin. PCI-27483 (0 and 90 mg/kg, s.c.) results in inhibition of tumor growth in CD1 nu/nu mice implanted with BxPC3 cells.

PCI27483 | PCI-27483 | PCI 27483

Angiogenesis

CDK

Coagulation factor

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871266-63-6

596.57

C26H24N6O9S

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (104.77 mM)

c1cc2c(cc1C(=N)N)[nH]c(c1cc(cc(c1O)c1c(ccc(c1)S(=O)(=O)N)O)CC(=O)NC(CC(=O)O)C(=O)O)n2

(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.

(-20℃)

With Ice Pack

≥ 2 years