A dual PDK1 and class I PI3K inhibitor
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NVP-BAG956

Item No. 24195

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α,α-dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
CAS Number
853910-02-8
Synonyms
  • BAG956
Molecular Formula
C28H21N5
Formula Weight
427.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 20 mg/ml
SMILES
CC1=NC2=C(N1C3=CC=C(C(C)(C)C#N)C=C3)C4=CC(C#CC5=CC=CN=C5)=CC=C4N=C2
InChi Code
InChI=1S/C28H21N5/c1-19-32-26-17-31-25-13-8-20(6-7-21-5-4-14-30-16-21)15-24(25)27(26)33(19)23-11-9-22(10-12-23)28(2,3)18-29/h4-5,8-17H,1-3H3
InChi Key
GVPAGJWVBUZHNQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $167

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    10 mg

    $255

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    Product Description

    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).1 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 = <100 nM).2 It induces cell cycle arrest at the G1 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).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stauffer, F., Maira, S.M., Furet, P., et al. Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. Bioor. Med. Chem. Lett. 18(3), 1027-1030 (2008).

    2. Weisberg, E., Banerji, L., Wright, R.D., et al. Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells. Blood 111(7), 3723-3734 (2008).