PF-3758309
Cat. No.:YN270210
CAS No. :898044-15-0
产品名称: | PF-3758309 |
CAS No.: | 898044-15-0 |
Chemical Name: | N-[(1S)-2-(dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide |
Synonyms: | PF-03758309 |
分子量: | 490.62 |
分子式: | C₂₅H₃₀N₈OS |
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 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | PF-3758309 是一种有效的、口服的、可逆的 ATP 竞争性PAK4抑制剂 (Kd= 2.7 nM;Ki=18.7 nM)。PF-3758309 具有 PAK4 抑制剂的预期细胞功能:抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。 |
IC50和靶点: | [{name:"PAK4:18.7 nM (Ki)"},{name: "PAK1:13.7 nM (Ki)"},{name: "PAK5:18.1 nM (Ki)"},{name: "PAK6:17.1 nM (Ki)"},{name: "PAK2:190 nM (IC50)"},{name: "PAK3:99 nM (IC50)"},{name: "PAK4:2.7 nM (Kd)"}] |
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Kumar, R., Gururaj, A.E., and Barnes, C.J.p21-activated kinases in cancerNat. Rev. Cancer6(6),459-471(2006)
Murray, B.W., Guo, C., Piraino, J., et al.Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growthProc. Natl. Acad. Sci. USA107(20),9446-9451(2010)