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PF-03758309 (hydrochloride) manufacturers
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| | PF-03758309 (hydrochloride) Basic information |
| Product Name: | PF-03758309 (hydrochloride) | | Synonyms: | PF-03758309 (hydrochloride);PF-3758309 hydrochloride;growth,PF3758309 hydrochloride,p21 activated kinases,proliferation,survival,signaling,PF 03758309,ATP-competitive,PF 3758309 hydrochloride,oncogenic,PF3758309,PF-03758309,PF03758309,PF 3758309,inhibit,tumor,PF-3758309,PAK,Apoptosis,Inhibitor;PF-03758309 Dihydrochloride;PF-3758309 hydrochloride, 10 mM in DMSO | | CAS: | 1279034-84-2 | | MF: | C25H31ClN8OS | | MW: | 527.09 | | EINECS: | | | Product Categories: | | | Mol File: | 1279034-84-2.mol |  |
| | PF-03758309 (hydrochloride) Chemical Properties |
| | PF-03758309 (hydrochloride) Usage And Synthesis |
| 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 |
| | PF-03758309 (hydrochloride) Preparation Products And Raw materials |
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