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BAG 956
- NVP-BAG956
- Soluble in DMSO
- MF: C28H21N5
- MW: 427.5
Description
BAG 956 is a potent, ATP-competitive dual PI3K and PDPK1 inhibitor with reported IC50 values of 56 nM for PI3K p110α, 444 nM for p110β, 34 nM for p110δ, 117 nM for p110γ and 240 nM for PDPK1.
PI3K and PDPK1 coordinate AKT pathway activation, growth factor signaling, survival and cancer cell proliferation. BAG 956 is used to interrogate PI3K isoform and PDPK1 contributions in vitro and in vivo.
Key Features
- ATP-competitive PI3K/PDPK1 inhibitor
- Inhibits multiple PI3K p110 isoforms
- Reported IC50 range: 34-444 nM across PI3K isoforms and 240 nM for PDPK1
- Useful for PI3K-AKT pathway dissection
Applications
- PI3K isoform kinase assays
- PDPK1 and AKT pathway studies
- Cancer signaling and survival models
- Growth factor pathway inhibitor profiling
More Information
| Parent CAS No. | 853910-02-8 |
|---|---|
| Chemical Name | 2-methyl-2-[4-(2-methyl-8-pyridin-3-ylethynyl-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile |
| SMILES | CC(C#N)(C1C=CC(N2C(C)=NC3C=NC4=CC=C(C#CC5C=NC=CC=5)C=C4C=32)=CC=1)C |
| MFCD | MFCD16618394 |
| InChi | 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 |
| InChiKey | GVPAGJWVBUZHNQ-UHFFFAOYSA-N |
| CID | 24882589 |
| Short Description | PI3K/PDK1 inhibitor |
References
- R Marone et al. Targeting Melanoma with Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors. Mol. Cancer Res. 2009, 7(4), 601-613.
- SM Maria, P Furet and F Stauffer. Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway. Future Med. Chem. 2009, 1(1), 137-155.
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