Alpelisib
Cat. No.:YN420202
产品名称: | Alpelisib |
CAS No.: | 1217486-61-7 |
Chemical Name: | (2S)-N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide |
Synonyms: | BYL-719 |
分子量: | 441.47 |
分子式: | C₁₉H₂₂F₃N₅O₂S |
SMILES: | CC(N=C(S1)NC(N2CCC[C@H]2C(N)=O)=O)=C1C3=CC(C(C)(C(F)(F)F)C)=NC=C3 |
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: | Alpelisib (BYL-719) 是有效,选择性的,具有口服活性的PI3Kα抑制剂。Alpelisib (BYL-719) 对 PIK3CA 突变癌具有靶向性。Alpelisib (BYL-719) 抑制 p110α、p110γ、p110δ、p110β 的IC50分别为 5 nM,250 nM,290 nM,1200 nM。具有抗肿瘤活性。 |
IC50和靶点: | [{name:"p110α:5 nM (IC50)"},{name: "p110γ:250 nM (IC50)"},{name: "p110δ:290 nM (IC50)"},{name: "p110β:1200 nM (IC50)"},{name: "p110α-H1047R:4 nM (IC50)"},{name: "p110α-E545K:4 nM (IC50)"}] |
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Fritsch, C., Huang, A., Chatenay-Rivauday, C., et al.Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trialsMol. Cancer Ther.13(5),1117-1129(2014)
Gritsman, K., Yuzugullu, H., Von, T., et al.Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110αJ. Clin. Invest.124(4),1794-1809(2014)
Elkabets, M., Vora, S., Juric, D., et al.mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancerSci. Transl. Med.5(196),196ra199(2013)