LKT Labs

Biochemicals for Life Science Research

PF-03758309 Dihydrochloride

PF-03758309 Dihydrochloride

Product ID P2000
Cas No. 1279034-84-2
Purity ≥99%, ≥99%ee
Product Unit SizeCostQuantityStock
1 mg $105.30 In stock
5 mg $180.30 In stock
25 mg $480.70 In stock
Bulk Quote

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Description

PF-03758309 is an ATP-competitive inhibitor of p21-activated kinase 4 (PAK4), a kinase typically upregulated in many cancers. This compound exhibits anticancer chemotherapeutic and anti-metastatic activities. Inhibition of PAK4 inhibits cell motility, proliferation, and survival in cellular models of cancer and suppresses tumor growth in animal models of cancer. PF-03758309 also inhibits fusion and migration of preosteoclasts, osteoclast differentiation, and podosome formation in cellular models of osteoclast-related disorders.

Product Info

Cas No.

1279034-84-2
Purity

≥99%, ≥99%ee
Formula

C25H30N8OS • 2HCl
Formula Wt.

563.55
IUPAC Name

N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide;hydrochloride
Synonym

PF-3758309 .2HCl
Solubility

Soluble in DMSO, water and alcohols.
Appearance

Off white to pale yellow powder

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

MSDS

P2000 MSDS PDF
Info Sheet

P2000 Info Sheet PDF

References

Choi SW, Yeon JT, Ryu BJ, et al. Repositioning Potential of PAK4 to Osteoclastic Bone Resorption. J Bone Miner Res. 2015 Jan 31. [Epub ahead of print]. PMID: 25640698.

Ryu BJ, Lee H, Kim SH, et al. PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings Mol Cell Biochem. 2014 Apr;389(1-2):69-77. PMID: 24366569.

Murray BW, Guo C, Piraino J, et al. Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51. PMID: 20439741.

www.clinicaltrials.gov/show/NCT00932126

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