PCI-27483 | CAS#871266-63-6 | factor VIIa inhibitor

MedKoo Cat#: 205574 | Name: PCI-27483

Description:

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

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

PCI-27483

CAS#871266-63-6

Theoretical Analysis

MedKoo Cat#: 205574

Name: PCI-27483

CAS#: 871266-63-6

Chemical Formula: C26H24N6O9S

Exact Mass: 596.1326

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
5mg	USD 110.00	Ready to ship
10mg	USD 180.00	Ready to ship
25mg	USD 400.00	Ready to ship
50mg	USD 700.00	Ready to ship
100mg	USD 1,250.00	Ready to ship
200mg	USD 2,250.00	Ready to ship

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Related CAS #

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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

More Info

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. .

Certificate of Analysis

View CoA: current batch, Lot#CRB70404

QC Data

View QC data: current batch, Lot#CRB70404

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

	Solvent	mg/mL	mM
Solubility
	DMSO	10.0	16.80

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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

1: Shrimp JH, Janiszewski J, Chen CZ, Xu M, Wilson KM, Kales SC, Sanderson PE, Shinn P, Schneider R, Itkin Z, Guo H, Shen M, Klumpp-Thomas C, Michael SG, Zheng W, Simeonov A, Hall MD. Suite of TMPRSS2 Assays for Screening Drug Repurposing Candidates as Potential Treatments of COVID-19. ACS Infect Dis. 2022 Jun 10;8(6):1191-1203. doi: 10.1021/acsinfecdis.2c00172. Epub 2022 Jun 1. PMID: 35648838; PMCID: PMC9172053. 2: Shrimp JH, Janiszewski J, Chen CZ, Xu M, Wilson KM, Kales SC, Sanderson PE, Shinn P, Itkin Z, Guo H, Shen M, Klumpp-Thomas C, Michael SG, Zheng W, Simeonov A, Hall MD. A Suite of TMPRSS2 Assays for Screening Drug Repurposing Candidates as Potential Treatments of COVID-19. bioRxiv [Preprint]. 2022 Feb 7:2022.02.04.479134. doi: 10.1101/2022.02.04.479134. Update in: ACS Infect Dis. 2022 Jun 10;8(6):1191-1203. doi: 10.1021/acsinfecdis.2c00172. PMID: 35169799; PMCID: PMC8845423. 3: Sun YJ, Velez G, Parsons DE, Li K, Ortiz ME, Sharma S, McCray PB Jr, Bassuk AG, Mahajan VB. Structure-based phylogeny identifies avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice. J Clin Invest. 2021 May 17;131(10):e147973. doi: 10.1172/JCI147973. PMID: 33844653; PMCID: PMC8121520. 4: Ramanathan RK, Thomas GW, Khorana AA, Shah S, Zhou C, Wong S, Cole G Jr, James D, Gabrail NY. A Phase 2 Study of PCI-27483, a Factor VIIa Inhibitor in Combination with Gemcitabine for Advanced Pancreatic Cancer. Oncology. 2019;96(4):217-222. doi: 10.1159/000495988. Epub 2019 Mar 7. PMID: 30844808; PMCID: PMC6492608. 5: Gómez-Outes A, Suárez-Gea ML, Lecumberri R, Rocha E, Pozo-Hernández C, Vargas-Castrillón E. New parenteral anticoagulants in development. Ther Adv Cardiovasc Dis. 2011 Feb;5(1):33-59. doi: 10.1177/1753944710387808. Epub 2010 Nov 2. PMID: 21045018.