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PCI-27483

Names

[ CAS No. ]:
871266-63-6

[ Name ]:
PCI-27483

[Synonym ]:
L-Aspartic acid, N-[2-[5-[6-(aminoiminomethyl)-1H-benzimidazol-2-yl]-5'-(aminosulfonyl)-2',6-dihydroxy[1,1'-biphenyl]-3-yl]acetyl]-
L-Aspartic acid, N-[[5-[5-(aminoiminomethyl)-1H-benzimidazol-2-yl]-5'-(aminosulfonyl)-2',6-dihydroxy[1,1'-biphenyl]-3-yl]acetyl]-
(S)-2-[[2-[5-(5-Carbamimidoyl-1H-benzimidazol-2-yl)-6,2'-dihydroxy-5'-sulfamoylbiphenyl-3-yl]acetyl]amino]succinic acid
PCI27483/PCI-27483
N-{[5-(5-Carbamimidoyl-1H-benzimidazol-2-yl)-2',6-dihydroxy-5'-sulfamoyl-3-biphenylyl]acetyl}-L-aspartic acid
PCI-27483

Biological Activity

[Description]:

PCI-27483 is a FVIIa/tissue factor inhibitor, with antitumour effects.

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Cancer

[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].

[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].

[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.


[Related Small Molecules]

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Molecular Formula ]:
C26H24N6O9S

[ Molecular Weight ]:
596.569

[ Exact Mass ]:
596.132568

[ PSA ]:
291.25000

[ LogP ]:
-0.74

[ Index of Refraction ]:
1.775

Related Compounds