产品信息
抗原名称
PI3Kδ ,PI3Kα ,PI3Kγ ,PI3Kβ
商品描述
AZD8835是一种有效的选择性PI3Kδ 和PI3Kα抑制剂, IC50值分别为5.7 nM 和 6.2 nM, 选择性优于PI3Kβ (IC50为 431 nM)和 PI3Kγ (IC50为 90 nM)。
分子量
469.54
纯度
＞98%
可溶性
DMSO Solubility: 93 mg/mL (198.06 mM)
In vitro(体外研究)
AZD8835 is a potent inhibitor of PI3Kα (wild type, E545K and H1047R mutations) and PI3Kδ with excellent selectivity vs. PI3Kβ, PI3Kγ and an excellent general kinase selectivity. AZD8835 is a potent inhibitor of p-Akt in cells sensitive to PI3Kα inhibition (IC50=0.057 μM in PIK3CA mutant human breast ductal carcinoma BT474 cell line) and in cells sensitive to PI3Kδ inhibition (IC50=0.049 μM in JeKo-1 B cell line), but not to cells sensitive to PI3Kβ inhibition (IC50=3.5 μM in PTEN null breast adenocarcinoma MDA-MB-468 cell line) or PI3Kγ inhibition (IC50=0.53 μM in monocytic RAW264 cell line).
In vivo(体内研究)
AZD8835 has antitumor efficacy in corresponding breast cancer xenograft models when dosed continuously and displays high metabolic stability and suitable physical properties for oral administration.
背景
别名
AZD-8835
分子式
C22H31N9O3
CAS号
1620576-64-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
本文来自投稿，不代表本人立场，如若转载，请注明出处：http://www.iamyjet.com/article/21591.html