产品描述:
NVP-BAG956 is a dual inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 245 nM) and class I phosphatidylinositol 3-kinase catalytic subunits (PI3Ks; IC50s = 56, 446, 35, and 117 nM for p110α, p110β, p110δ, and p110γ, respectively).{36931} It inhibits phosphorylation of T308-PKB (IC50 = 45 nM) in and proliferation of U87MG cells (EC50 = 143 nM). NVP-BAG956 decreases cell viability in a panel of human leukemia cell lines (IC50s = 1 phase in MOLM-14 cells and reduces colony formation by patient-derived acute myeloid leukemia (AML) cells. NVP-BAG956 (75 mg/kg) reduces tumor burden in mice injected with 32D.p210-luc+cells when administered in combination with everolimus (Item No. 11597).