CAL-101

一种细胞渗透性PI3K催化亚基p110δ抑制剂(IC50=2.5nM)，对其他PI3KI类酶具有40至300倍的选择性（p110α、β和γ的IC50分别为820、565和89nM）；阻断恶性B细胞系和患者原发性肿瘤细胞中的组成性PI3K信号传导，导致Akt和其他下游效应物的磷酸化降低、聚（ADP-核糖）聚合酶增加和细胞凋亡。A cell permeable inhibitor of the PI3K catalytic subunit p110δ (IC50 = 2.5 nM) that demonstrates 40- to 300-fold selectivity against other PI3K class I enzymes (IC50s = 820, 565, and 89 nM for p110α, β, and γ, respectively); blocks constitutive PI3K signaling in malignant B-cell lines and primary patient tumor cells, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and apoptosis.