NVP-BAG956

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NVP-BAG956 (BAG956) 是一种有效的 PDK-1/PI3K 双重抑制剂。

NVP-BAG956 (BAG956) is a potent, dual PDK-1/PI3K inhibitor with IC50 of 245/56/446/35/117 nM for PDK1/p110α/p110β/p110δ/p110γ, respectively; inhibits p-T308-PKB U87MG cells with IC50 of 45 nM in ELISA assays, shows anti-proliferative activity with EC50 of 143 nM; blocks AKT phosphorylation induced by BCR-ABL–, and induces apoptosis of BCR-ABL–expressing cell lines and patient bone marrow cells at concentrations that also inhibit PI3K signaling; demonstrates against BCR-ABL expressing cells both in vitro and in vivo, BAG956 is effective against mutant FLT3-expressing cell lines and AML patient bone marrow cells.

NVP-BAG956 also inhibits PDK1 with an IC50 of 240/260 nM. NVP-BAG956 also inhibits VEGFR1 with an IC50 of 2.56±0.56 μM. NVP-BAG956 blocks phosphorylation of PKB/Akt in A2058 cells with an IC50 value of 67±25 nM. Inhibition of PKB/Akt phosphorylation correlated with loss of A2058 cell proliferation for NVP-BAG956 (IC50=290±20 nM). In the presence of NVP-BAG956, A2058 cells are only able to exit G2-M and then remain in G1. The p27 Kip1 expression is clearly induced by NVP-BAG956 in A2058 cells but not in C32 cells.

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BAG 956

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

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853910-02-8

427.5

C28H21N5

>98% (HPLC)

10 mM in DMSO

c1cc(c(cc1CCCNCCCO)C(=O)NCC23CC4CC(C2)CC(C4)C3)Cl

Benzeneacetonitrile, α,α-dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-

(-20℃)

With Ice Pack

≥ 2 years