PCI-27483

Modify Date: 2024-01-06 18:16:14

PCI-27483 Structure
PCI-27483 structure
Common Name PCI-27483
CAS Number 871266-63-6 Molecular Weight 596.569
Density 1.7±0.1 g/cm3 Boiling Point N/A
Molecular Formula C26H24N6O9S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PCI-27483


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

 Names

Name L-Aspartic acid, N-[2-[5-[6-(aminoiminomethyl)-1H-benzimidazol-2-yl]-5'-(aminosulfonyl)-2',6-dihydroxy[1,1'-biphenyl]-3-yl]acetyl]
Synonym More Synonyms

 PCI-27483 Biological Activity

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

 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

 Synonyms

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
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