CAL-101 是 p110δ 的选择性抑制剂(IC50:2.5 nM;在无细胞试验中);显示对 p110δ 的选择性比 p110α/β/γ 高 40 到 300 倍,对 p110δ 的选择性比 C2β、hVPS34、DNA-PK 和 mTOR 高 400 到 4000 倍。
产品描述
CAL-101 is a selective inhibitor of p110δ(IC50 : 2.5 nM; in cell-free assays); shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.
体外活性
CAL-101 blocked constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis[1].
Cas No.
1146702-54-6
分子式
C22H18FN7O
分子量
415.42
别名
GS-1101;Idelalisib
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years