870281-82-6

溶解度:unknown

储存条件:-20C 2 years

生物活性

CAL-101 is a potent PI3K p110 inhibitor with an IC50 of 65 nM. 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. CAL-101 has 40 to 300-fold selectivity compared to other PI3K isoforms. In vitro studies of 0.1 to 10 µM CAL-101 showed inhibition of pAKT expression and/or apoptotic effects against primary chronic lymphocytic leukemia (CLL) and acute myeloid leukemia (AML) cells and against a range of leukemia and lymphoma cell lines.

参考文献

[1] http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=65&abstractID=34213 [2] Lannutti BJ et al. Blood. 2011 Jan 13;117(2):591-4.