PCI-27483

SKU: orb1223017

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.

Key Properties

• CAS Number: 871266-63-6
• MW: 596.57
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₄N₆O₉S
• SMILES: 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
• Target: CDK
• Solubility: In Vitro: DMSO : 62.5 mg/mL (104.77 mM)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PCI27483 | PCI-27483 | PCI 27483

Quick Database Links

Gene Symbol

CDK