| Identification | Back Directory | [Name]
PF-03758309 (hydrochloride) | [CAS]
1279034-84-2 | [Synonyms]
PF-3758309 hydrochloride
PF-03758309 (hydrochloride) | [Molecular Formula]
C25H31ClN8OS | [MOL File]
1279034-84-2.mol | [Molecular Weight]
527.09 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
PF-3758309 hydrochloride (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models[1]. | Animal Model: | Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors)[1] | | Dosage: | 7.5-30 mg/kg | | Administration: | Oral administration; twice daily for 9-18 days | | Result: | Significant tumor growth inhibition (TGI) in HCT116 and A549 models. |
| [IC 50]
PAK4: 18.7 nM (Ki); PAK1: 13.7 nM (Ki); PAK5: 18.1 nM (Ki); PAK6: 17.1 nM (Ki); PAK2: 190 nM (IC50); PAK3: 99 nM (IC50); PAK4: 2.7 nM (Kd) | [References]
[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. DOI:10.1073/pnas.0911863107
[2] Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70. DOI:10.3410/B2-70
[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. DOI:10.1007/s11010-013-1928-8 |
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