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NVP-BBD130
- BBD 130
- Moderately soluble in DMSO
- MF: C28H21N5O
- MW: 443.5
Description
NVP-BBD130 is an orally active dual PI3K/mTOR inhibitor with reported IC50 values of 72, 2336, 201 and 382 nM for PI3K p110 α, β, δ and γ isoforms, respectively. It inhibits the PI3K/mTOR pathway like NVP-BEZ235 and efficiently attenuates growth and proliferation of melanoma primary tumors and metastasis.
The PI3K/AKT/mTOR axis controls cell survival, metabolism, protein synthesis and tumor growth. NVP-BBD130 is useful for studying pathway blockade, kinase selectivity and antitumor pharmacology in models dependent on PI3K or mTOR signaling.
Key Features
- Dual PI3K/mTOR pathway inhibitor
- Reported activity against multiple class I PI3K isoforms
- Suppresses growth and survival signaling downstream of PI3K
- Useful for dissecting PI3K versus mTOR pathway contributions
Applications
- PI3K/AKT/mTOR signaling research
- Oncology pathway-dependence studies
- Kinase inhibitor profiling
- Tumor cell proliferation assays
More Information
| Parent CAS No. | 853910-61-9 |
|---|---|
| Chemical Name | 2-Methyl-2-[4-(3-methyl-2-oxo-8-pyridin-3ylethynyl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile |
| SMILES | C1(C#CC2C=C3C4N(C5C=CC(C(C)(C)C#N)=CC=5)C(=O)N(C)C=4C=NC3=CC=2)C=NC=CC=1 |
| MFCD | MFCD17215199 |
| InChi | InChI=1S/C28H21N5O/c1-28(2,18-29)21-9-11-22(12-10-21)33-26-23-15-19(6-7-20-5-4-14-30-16-20)8-13-24(23)31-17-25(26)32(3)27(33)34/h4-5,8-17H,1-3H3 |
| InChiKey | ISHNPDWTQUXPSY-UHFFFAOYSA-N |
| CID | 11751126 |
| Short Description | PI3K/mTOR 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.
- F Stauffer et al. Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. Bioorg. Med. Chem. Lett. 2008, 18, 1027-1030.
- 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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