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NVP-BAG956

Chemical Structure : NVP-BAG956

CAS No.: 853910-02-8

NVP-BAG956 (BAG956, BAG 956)

Catalog No.: PC-43502Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.
NVP-BAG956 inhibits p-T308-PKB U87MG cells with IC50 of 45 nM in ELISA assays, shows anti-proliferative activity with EC50 of 143 nM.
NVP-BAG956 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.
NVP-BAG956 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.

Physicochemical Properties

M.Wt 427.50
Formula C28H21N5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Stauffer F, et al. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1027-30.

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