产品描述:
AZD 8186 is a selective PI3Kβ/δ inhibitor that exhibits IC50 values of 3, 17, and 752 nM for PI3Kβ, δ, and α, respectively, in cells sensitive to isoform-specific PI3K inhibition.{33193,33194} It shows no significant binding against a panel of 442 other kinases when tested at a concentration of 10 µM and exhibits high oral efficacy in mouse cancer models.{33193} AZD 8186 inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency, and inhibits growth of prostate and triple negative breast cancer tumors in vivo, both as a single agent and in combination with docetaxel (Item No. 11637).{33194}