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Cat. No. Name Size Price Add Cart
KI2704PF-375830910 mg$283.4
PF-375830950 mg$915.2
PF-3758309100 mg$1544.4

Chemical Characteristic

Product NamePF-3758309
SynonymsPF 3758309; PF3758309
CAS No.898044-15-0
Molecular Weight 490.6237
FormulaC25H30N8OS
Chemical NameN-[(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
Smilesn1[nH]c2c(c1Nc1c3c(nc(n1)C)ccs3)CN(C2(C)C)C(=O)NC(CN(C)C)c1ccccc1
Chemical Structure

Biological activities

PF-3758309 is a potent and reversible ATP-competitive inhibitor of PAK4. PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 and anchorage-independent growth of a panel of tumor cell lines with IC50s of 1.3 and 4.7 nM, respectively. In vitro in A549 cells, PF-3758309 inhibits cellular proliferation and anchorage-independent growth with IC50s of 20 and 27 nM, respectively. In vivo, in tumor models, PF-3758309 inhibits PAK4-dependent pathways in proteomic studies and regulates functional activities related to cell proliferation and survival.[1]

Protocols

In vitro, PF-3758309 is dissolved in DMSO.[1]

References

[1]Brion W, et al. Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc Natl Acad Sci. 2010, 107 (20): 9446-9451.

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