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BEZ 235
- NVP-BEZ235 - Dactolisib
- Moderately soluble in DMSO
- MF: C30H23N5O
- MW: 469.54
Description
BEZ 235 (Dactolisib) is an orally active dual PI3K/mTOR inhibitor that targets phosphoinositide 3-kinase signaling and mTOR kinase activity.
The PI3K-AKT-mTOR pathway regulates growth factor signaling, proliferation, survival, metabolism and tumor progression. BEZ 235 is used to study pathway blockade and antiproliferative responses in cancer models.
Key Features
- Dual PI3K/mTOR kinase inhibitor
- Orally active pharmacology profile
- Blocks PI3K-AKT-mTOR pathway signaling
- Reported antiproliferative activity in tumor model systems
Applications
- PI3K and mTOR kinase assays
- AKT-mTOR pathway studies
- Cancer cell proliferation research
- Growth factor signaling and survival pathway models
More Information
| Parent CAS No. | 915019-65-7 |
|---|---|
| Chemical Name | 2-Methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile |
| SMILES | C1(C2C=C3C=CC=CC3=NC=2)C=C2C3N(C4C=CC(C(C)(C)C#N)=CC=4)C(=O)N(C)C=3C=NC2=CC=1 |
| MFCD | MFCD10565944 |
| InChi | InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3 |
| InChiKey | JOGKUKXHTYWRGZ-UHFFFAOYSA-N |
| CID | 11977753 |
| Short Description | PI3K/mTOR inhibitor |
References
- JC Verheijen, A Zask. Phosphatidylinositol 3-kinase (PI3K) inhibitors as anticancer drugs. Drugs Fut 2007, 32(6), 537.
- SM Maira et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther 2008, 7(7), 1851–1863.
- 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.
- SM Brachmann et al. Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells. PNAS, 2009, 106 (52), 22299-22304.
- A list of citations for Axon Medchem product Axon 1281 - BEZ 235.
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