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PF-3758309 hydrochloride

Catalog No. T4230   CAS 1279034-84-2
Synonyms: PF-03758309 hydrochloride

PF-3758309 hydrochloride (PF-03758309 hydrochloride) , is a PAK4 inhibitor, is also a n orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PF-3758309 hydrochloride binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

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PF-3758309 hydrochloride Chemical Structure
PF-3758309 hydrochloride, CAS 1279034-84-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 50.00
5 mg In stock $ 74.00
10 mg In stock $ 120.00
25 mg In stock $ 191.00
50 mg In stock $ 352.00
100 mg In stock $ 553.00
1 mL * 10 mM (in DMSO) In stock $ 116.00
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Purity: 100%
Purity: 98.11%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-3758309 hydrochloride (PF-03758309 hydrochloride) , is a PAK4 inhibitor, is also a n orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PF-3758309 hydrochloride binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.
Targets&IC50 PAK3:99 nM (IC50), PAK2:190 nM (IC50), PAK1:13.7 nM (Ki), PAK4:18.7 nM (Ki), PAK4:2.7 nM (Kd), PAK6:17.1 nM (Ki), PAK5:18.1 nM (Ki)
Synonyms PF-03758309 hydrochloride
Molecular Weight 527.08
Formula C25H31ClN8OS
CAS No. 1279034-84-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (85.37 mM)

TargetMolReferences and Literature

1. Briz V, Baudry M. Estrogen Regulates Protein Synthesis and Actin Polymerization in Hippocampal Neurons through Different Molecular Mechanisms. Front Endocrinol (Lausanne). 2014 Feb 25;5:22. doi: 10.3389/fendo.2014.00022. eCollection 2014. PubMed PMID: 24611062; PubMed Central PMCID: PMC3933789. 2. Fu X, et al. PAK4 confers cisplatin resistance in gastric cancer cells via PI3K/Akt- and MEK/Erk-dependent pathways. Biosci Rep. 2014 Jan 29. [Epub ahead of print] PubMed PMID: 24471762; PubMed Central PMCID: PMC3941610. 3. Ryu BJ, 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. doi: 10.12007/s112010-2013-1928-8. Epub 2013 Dec 24. PubMed PMID: 24366569. 4. Gao J, et al. Substrate and inhibitor specificity of the type 2 p21-activated kinase, PAK6. PLoS One. 2013 Oct 28;8(10):e77818. doi: 10.1371/journal.pone.20077818. eCollection 2013. PubMed PMID: 24204982; PubMed Central PMCID: PMC38120134. 5. Itakura A, et al. p21-Activated kinase (PAK) regulates cytoskeletal reorganization and directional migration in human neutrophils. PLoS One. 2013 Sep 3;8(9):e73063. doi: 10.1371/journal.pone.20073063. eCollection 2013. PubMed PMID: 242019894; PubMed Central PMCID: PMC3760889.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Inhibitor Library Anti-Cancer Compound Library Apoptosis Compound Library Bioactive Compound Library

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Keywords

PF-3758309 hydrochloride 1279034-84-2 Apoptosis Cytoskeletal Signaling PAK growth PF3758309 hydrochloride PF 3758309 Hydrochloride p21 activated kinases proliferation survival PF-3758309 Hydrochloride PF-03758309 hydrochloride signaling PF 03758309 ATP-competitive PF 3758309 hydrochloride oncogenic PF03758309 Hydrochloride PF3758309 PF-03758309 PF03758309 PF 3758309 PF-03758309 Hydrochloride inhibit tumor PF3758309 Hydrochloride PF-3758309 PF 03758309 Hydrochloride Inhibitor inhibitor

 

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