1146702-54-6
中文名稱
CAL-101
英文名稱
CAL-101
CAS
1146702-54-6
分子式
C22H18FN7O
分子量
415.423
MOL 文件
1146702-54-6.mol
更新日期
2024/05/20 09:19:54
1146702-54-6 結(jié)構(gòu)式
基本信息
中文別名
艾代拉里斯雜質(zhì)艾代拉里斯雜質(zhì)A
英文別名
IdelalisibGS-1101, Idelalisib
CAL-101 (GS-1101, Idelalisib)
5-fluoro-3-phenyl-2-((1s)-1-(1h-purin-6-ylamino)ethyl)-4(3h)...
所屬類別
生物化工：抑制劑應(yīng)用領(lǐng)域
用途一
Idelalisib is an orally available selective and potent phosphatidylinositol
3-kinase δ (PI3 Kδ) inhibitor originally developed
by Calistoga Pharmaceuticals, which was acquired by Gilead in
April 2014. In July 2014, the drug was approved in the USA for
the treatment of relapsed chronic lymphocytic leukemia as well
as several oncology orphan drug designations. Since idelalisib
specifically inhibits PI3Kd, which is expressed primarily in bloodcell
lineages, the therapeutic effect is localized, limiting interference
with PI3K isoform signaling that is critical to normal function
of healthy cells.常見(jiàn)問(wèn)題列表
生物活性
CAL-101是一種有效的選擇性的p110δ抑制劑，IC50為2.5nM，比作用于其他I類PI3K酶(抑制p110α，p110β和p110γ；IC50分別為820，565和89nM)選擇性高40到300倍。