1279034-84-2
Chemical Structure
PF-3758309 hydrochloride
Synonym(s): PF-03758309 hydrochloride
- CAS No.: 1279034-84-2
- Formula:C25H31ClN8OS
- Molecular Weight:527.08
IUPAC Name: (S)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-((2-methylthieno[3,2-d]pyrimidin-4-yl)amino)-2,6-dihydropyrrolo[3,4-c]pyrazole-5(4H)-carboxamide hydrochloride
InChIKey: DZSGSCZKFHGJNK-FSRHSHDFSA-N
SMILES: O=C(N1C(C)(C)C2=NNC(NC3=C4C(C=CS4)=NC(C)=N3)=C2C1)N[C@@H](C5=CC=CC=C5)CN(C)C.[H]Cl
Biological Activity: PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride 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].
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PF-3758309 hydrochloride | PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation. | |||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70. [Content Brief]
- [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. [Content Brief]
Keywords
