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PF-3758309

CAT: 0804-HY-13007-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-13007-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM) . PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3].
CAS Number
898044-15-0
Product Name Alternative
PF-03758309
UNSPSC
12352005
Hazard Statement
H302, H317
Target
Apoptosis; PAK
Type
Reference compound
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/PF-3758309.html
Concentration
10mM
Purity
99.79
Solubility
DMSO : ≥ 100 mg/mL
Smiles
CC1=NC2=C(SC=C2)C(NC3=NNC4=C3CN(C(N[C@@H](C5=CC=CC=C5)CN(C)C)=O)C4(C)C)=N1
Molecular Formula
C25H30N8OS
Molecular Weight
490.62
Precautions
H302, H317
References & Citations
[1]Murray, Brion W., et al. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proceedings of the National Academy of Sciences of the United States of America (2010), 107 (20), 9446-9451, S94|[2]Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70.|[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.|[4]Pitts TM, et al. Association of the epithelial-to-mesenchymal transition phenotype with responsiveness to the p21-activated kinase inhibitor, PF-3758309, in colon cancer models. Front Pharmacol. 2013 Mar 28;4:35.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
PAK1; PAK2; PAK3; PAK4; PAK5; PAK6

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