PCI-27483
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205574

CAS#: 871266-63-6

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.


Chemical Structure

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PCI-27483
CAS# 871266-63-6

Theoretical Analysis

MedKoo Cat#: 205574
Name: PCI-27483
CAS#: 871266-63-6
Chemical Formula: C26H24N6O9S
Exact Mass: 596.13255
Molecular Weight: 596.57
Elemental Analysis: C, 52.35; H, 4.05; N, 14.09; O, 24.14; S, 5.37

Price and Availability

Size Price Availability Quantity
5.0mg USD 90.0 Ready to ship
10.0mg USD 150.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 850.0 Ready to ship
200.0mg USD 1450.0 Ready to ship
500.0mg USD 2150.0 Ready to ship
1.0g USD 3850.0 2 Weeks
2.0g USD 5950.0 2 Weeks
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Synonym: PCI27483; PCI-27483; PCI 27483.

IUPAC/Chemical Name: (S)-2-(2-(5-(5-carbamimidoyl-1H-benzo[d]imidazol-2-yl)-2',6-dihydroxy-5'-sulfamoyl-[1,1'-biphenyl]-3-yl)acetamido)succinic acid.

InChi Key: WDJHHCAKBRKCLW-IBGZPJMESA-N

InChi Code: InChI=1S/C26H24N6O9S/c27-24(28)12-1-3-17-18(8-12)32-25(31-17)16-6-11(7-21(34)30-19(26(38)39)10-22(35)36)5-15(23(16)37)14-9-13(42(29,40)41)2-4-20(14)33/h1-6,8-9,19,33,37H,7,10H2,(H3,27,28)(H,30,34)(H,31,32)(H,35,36)(H,38,39)(H2,29,40,41)/t19-/m0/s1

SMILES Code: 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

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.0 16.8

Preparing Stock Solutions

The following data is based on the product molecular weight 596.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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



Additional Information

Pharmacyclics’s Factor VIIa inhibitor PCI-27483 is a novel first-in-human small molecule inhibitor that selectively targets FVIIa. As an inhibitor of FVIIa, PCI-27483 has two potential mechanisms of action: 1) inhibition of intracellular signaling involved in tumor growth and metastases and 2) inhibition of early coagulation processes associated with thromboembolism.
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