| 应用 |
A potent PI3K p110δ inhibitor |
| 产品介绍 |
CAL-101 (Idelalisib, GS-1101)是一种选择性p110δ抑制剂，IC50为2.5 nM；作用于p110δ比作用于p110α/β/γ选择性高40到300倍，作用于p110δ比作用于C2β， hVPS34， DNA-PK和mTOR选择性高400到4000倍。Phase 3。 |
| 备注 |
CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. P |
| 生化机理 |
CAL-101 (GS-1101) is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 nM. This compound induces selective cytotoxicity in CLL cells and is independent of IgVH mutational status. CAL--101 also acts as an antagonist in CD40L-mediated CLL cell survival. |
| 别名 |
Idelalisib; GS-1101;5-氟-3-苯基-2-[(1S)-1-(9H-嘌呤-6-基氨基)丙基]-4(3H)-喹唑啉酮;Idelalisib; GS-1101;(S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one |
