AZD1208 hydrochloride 是一种有效的,具有口服活性的,具有高度选择性的Pim抑制剂。
产品描述
AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor [1].
体外活性
AZD1208 hydrochloride shows good antiproliferative activity in a megakaryoblastic leukemia cell line, MOLM-16, with GI 50 values less than 100 nM [1]. AZD1208 hydrochloride (10 μM) inhibits the growth of Ramos cells, and at 1 μM, strongly inhibits PIM kinases in all cells at 1 μM. AZD1208 hydrochloride induces apoptosis, and PIM2 knockdown is mainly associated with an alteration of the cell cycle [2]. The combination of AZD1208 hydrochloride 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].
Cas No.
1621866-96-3
分子式
C21H22ClN3O2S
分子量
415.94
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years