AZD-5438
Cat. No.:YN290002
CAS No. :602306-29-6
产品名称: | AZD-5438 |
CAS No.: | 602306-29-6 |
Chemical Name: | 4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine |
Synonyms: | AZD5438 |
分子量: | 371.46 |
分子式: | C₁₈H₂₁N₅O₂S |
SMILES: | O=S(C1=CC=C(NC2=NC(C3=CN=C(N3C(C)C)C)=CC=N2)C=C1)(C)=O |
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: | AZD-5438 是有效的CDK1,CDK2,CDK9抑制剂,IC50值分别为 16 nM, 6 nM, 20 nM。AZD-5438 对 GSK3β,CDK5,CDK6 的抑制作用较弱。 |
IC50和靶点: | [{name:"cdk2-cyclin E:6 nM (IC50)"},{name: "cdk2-cyclin A:45 nM (IC50)"},{name: "cdk5-p25:14 nM (IC50)"},{name: "cdk1-cyclin B1:16 nM (IC50)"},{name: "cdk9-cyclin T:20 nM (IC50)"},{name: "cdk6-cyclin D3:21 nM (IC50)"},{name: "cdk4-cyclin D1:449 nM (IC50)"},{name: "cdk7-cyclin H:821 nM (IC50)"}] |
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Byth, K.F., Thomas, A., Hughes, G., et al.AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenograftsMol. Cancer. Ther.8(7),1856-1866(2009)
Raghavan, P., Tumati, V., Yu, L., et al.AZD5438, an inhibitor of Cdk1, 2, and 9, enhances the radiosensitivity of non-small cell lung carcinoma cellsInt. J. Radiat. Oncol. Biol. Phys.84(4),e507-e514(2012)
Dickson, M.A., and Schwartz, G.K.Development of cell-cycle inhibitors for cancer therapyCurr. Oncol.16(2),36-43(2009)