PCI-27483

Description

Background Information:

PCI-27483 is a potent and selective small-molecule inhibitor of
activated factor VII (factor VIIa). 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,
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. In addition, this agent
inhibits both the extrinsic and intrinsic coagulation cascades,
preventing blood clot formation. TF, a blood protein overexpressed on
the cell surface of a variety of tumor cell types, may correlate with
poor prognosis; PAR-2 (also known as thrombin receptor-like 1) is a G
protein-coupled receptor (GPCR) and a protease-activated receptor.

Reference:

1. Manufacture, compositions and uses of coagulation factor VIIa
modulator, By Loury, David; Purro, Norbert, From PCT Int. Appl. (2009),
WO 2009052323 A2 20090423.

APIM050267: PCI-27483

CAS No.: 871266-63-6.
Molecular Formula: C₂₆H₂₄N₆O₉S ? 5xH₂O.
Molecular Weight: 686.6.
Purity: 99.5% (HPLC at 254 nm).
QC: HPLC, ¹HNMR and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.

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