A-443654
Cat. No.:YN420048
产品名称: | A-443654 |
CAS No.: | 552325-16-3 |
Chemical Name: | αS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-1H-indole-3-ethanamine |
Synonyms: | A 443654;A443654 |
分子量: | 397.47 |
分子式: | C₂₄H₂₃N₅O |
SMILES: | N[C@H](COC1=CN=CC(C2=CC3=C(NN=C3C)C=C2)=C1)CC4=CNC5=CC=CC=C54 |
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: | A-443654 是一种有效的pan-Akt抑制剂,以同等效力抑制Akt1,Akt2,和Akt3,Ki值均为 160 pM。 |
IC50和靶点: | [{name:"Akt1:160 pM (Ki)"},{name: "Akt2:160 pM (Ki)"},{name: "Akt3:160 pM (Ki)"},{name: "PKA:6.3 nM (Ki)"},{name: "PKCγ:24 nM (Ki)"},{name: "PKCδ:33 nM (Ki)"},{name: "KDR:3.1 μM (Ki)"},{name: "cKIT:1.2 μM (Ki)"},{name: "SRC:2.6 μM (Ki)"},{name: "Flt1:3.6 μM (Ki)"},{name: "CDK2:24 nM (Ki)"},{name: "ERK2:340 nM (Ki)"},{name: "GSK3β:41 nM (Ki)"},{name: "CK2:2.4 μM (Ki)"},{name: "Chk1:2.3 μM (Ki)"},{name: "RSK2:11 nM (Ki)"},{name: "MAPK-AP2:3.3 μM (Ki)"}] |
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Luo, Y., Shoemaker, A.R., Liu, X., et al.Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivoMol. Cancer Ther.4(6),977-968(2005)
Liu, X., Shi, Y., Woods, K.W., et al.Akt inhibitor a-443654 interferes with mitotic progression by regulating aurora a kinase expressionNeoplasia10(8),828-837(2008)
Han, E.K., Leverson, J.D., McGonigal, T., et al.Akt inhibitor A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibitionOncogene26(38),5655-5661(2007)