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PCI-27483

  Cat. No.:  DC8844   Featured
Chemical Structure
871266-63-6
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More than 5000 active chemicals with high quality for research!
Field of application
PCI-27483 is a selective small molecule inhibitor of activated coagulation factor VII (FVIIa), which is in preclinical development as a novel anti-cancer agent.
Cas No.: 871266-63-6
Chemical Name: (S)-2-(2-(5-(5-carbamimidoyl-1H-benzo[d]imidazol-2-yl)-2',6-dihydroxy-5'-sulfamoylbiphenyl-3-yl)acetamido)succinic acid
Synonyms: PCI27483,PCI-27483,PCI 27483
SMILES: 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
Formula: C26H24N6O9S
M.Wt: 596.57
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: PCI-27483 is a FVIIa/tissue factor inhibitor, with antitumour effects.
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[1]. PCI-27483 (0 and 90 mg/kg, s.c.) results in inhibition of tumor growth in CD1 nu/nu mice implanted with BxPC3 cells[2].
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[2].
References: [1]. Gómez-Outes A, et al. New parenteral anticoagulants in development. Ther Adv Cardiovasc Dis. 2011 Feb;5(1):33-59. [2]. Julia Prescott, et al. PCI-27483, a small molecule inhibitor of Factor VIIa, inhibits growth of BxPC3 pancreatic adenocarcinoma xenograft tumors. Cancer Research May 2008 Volume 68, Issue 9 Supplement.
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