(2S)-N1-[4-甲基-5-[2-(2,2,2-三氟-1,1-二甲基乙基)-4-吡啶基]-2-噻唑基]-1,2-吡咯烷二甲酰胺_详细资料

产品信息

CAS号： 1217486-61-7 供应商：上海经科化学科技有限公司数量：期货2-3周英文名： Alpelisib Free Base 保质期：＞1年保存条件：见说明书规格： 5mg

供应商：上海经科化学科技有限公司

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本试剂((2S)-N1-[4-甲基-5-[2-(2,2,2-三氟-1,1-二甲基乙基)-4-吡啶基]-2-噻唑基]-1,2-吡咯烷二甲酰胺)
仅供科研实验使用,不得用于其他用途！

简介：
货号：LC2-A-4477
名称：(2S)-N1-[4-甲基-5-[2-(2,2,2-三氟-1,1-二甲基乙基)-4-吡啶基]-2-噻唑基]-1,2-吡咯烷二甲酰胺
别名：Alpelisib Free Base
C A S ：1217486-61-7
分子量：441.47
分子式：C19H22F3N5O2S
纯度：HPLC/TLC:>99%
说明：
文献：Alpelisib, also known as BYL719, is a potent and selective phosphatidylinositol-3 kinase [alpha] inhibitor. It inhibited P110[alpha], p110[beta], p110[delta], and p110[gamma] with IC50 values of 5 nM, 1.2 µM, 0.29 µM and 0.25 µM, respectively, in biochemical assays. It inhibited the Akt phosphorylation with IC50 values of 74 nM in Rat1-myr-p110[alpha] cells, 2.2 µM in Rat1-myr-p110[beta] cells, and 1.2 µM in Rat1-myr-p110[delta] cells. Furet P., et al. "Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation." Bioorg. Med. Chem. Lett. 23: 3741-3748 (2013).Alpelisib showed dose- and time-dependent inhibition of PI3K[alpha] signaling in vivo and demonstrated robust anti-tumor response and tolerability in PIK3CA-dependent tumor models. Fritsch C., et al. "Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials." Mol. Cancer Ther. 13: 1117-1129 (2014).mTORC1 inhibition is necessary for sensitivity to PI3K p110[alpha] inhibition by alpelisib in PIK3CA-mutant breast cancer. Elkabets M., et al. "mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer." Sci. Transl. Med. 5: 196ra99 (2013).

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