tcsc1668 AZD1208

AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor.

In Vitro: AZD1208 shows good antiproliferative activity in a megakaryoblastic leukemia cell line, MOLM-16, with GI₅₀ values less than 100 nM^[1]. AZD1208 (10 μM) inhibits the growth of Ramos cells, and at 1 μM, strongly inhibits PIM kinases in all cell at 1 μM. AZD1208 induces apoptosis, and PIM2 knockdown is mainly associated with an alteration of the cell cycle^[2]. The combination of AZD1208 and AZD2014 rapidly activates AMPKα, a negative regulator of translation machinery through mTORC1/2 signaling in AML cells; profoundly inhibits AKT and 4EBP1 activation; and suppresses polysome formation^[3].