BEZ235 NVP-BEZ235(BEZ235)
2-methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile
CAS: 915019-65-7
Molecular Formula: C30H23N5O
BEZ235 NVP-BEZ235(BEZ235) - Names and Identifiers
BEZ235 NVP-BEZ235(BEZ235) - Physico-chemical Properties
| Molecular Formula | C30H23N5O |
| Molar Mass | 469.55 |
| Density | 1.299 |
| Melting Point | 288-289°C |
| Boling Point | 701.0±70.0 °C(Predicted) |
| Flash Point | 377.767°C |
| Solubility | Soluble in chloroform (1 mg/ml), 1-methyl-2-pyrrolidnone (2 mg/mL at 75 °C), DMSO (1.33 |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | White powder. |
| Color | White or off-white |
| pKa | 6.41±0.20(Predicted) |
| Storage Condition | Refrigerator |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 1 month. |
| Refractive Index | 1.705 |
| Physical and Chemical Properties | White-like to reddish powder |
| Use | A dual PI3K and mTOR inhibitor |
| In vitro study | BEZ235 significantly reduced the level of phosphorylation of the mTOR-activated kinase p70S6K. BEZ235 resulted in reduced S235/S236P-RPS6 levels with an IC50 of 6.5 nM. The activity of BEZ235 against mTOR was measured using a biochemical mTOR K-LISA assay with an IC50 of 20.7 nM. BEZ235 was slightly less active against its β paralogs, with an IC50 of 75 nM. In human tumor cells, the PI3K/Akt/mTOR pathway is often constitutively activated. BEZ235 blocks PI3K and mTOR kinase activity, acting by binding to the ATP binding groove of these enzymes. Treatment of PTEN-null cell lines PC3M and U87MG with gradually increasing concentrations of BEZ235 resulted in a dose-dependent decrease in cell proliferation with an average GI50 of 10-12 nM. BEZ235 is a catalytic inhibitor of mTORC1/2. |
| In vivo study | BEZ235 induced tumor regression (69%) without a statistically significant effect on body weight gain. Taken together, these preliminary in vivo efficacy results suggest that BEZ235 blocks disease progression when administered orally alone and enhances efficacy when combined with other anticancer drugs. |
BEZ235 NVP-BEZ235(BEZ235) - Introduction
BEZ235 (NVP-BEZ235, Dactolisib) ATP competitively inhibited PI3K and mTOR, p110α/γ/δ/β and mTOR(p70S6K), IC50 was 4 nM/5 nM/7 nM/75 nM/6 nM, respectively, and ATR was also inhibited, IC50 was 21 nM; But the inhibitory effect on Akt and PDK1 is weak.
Last Update：2022-10-16 17:30:06
BEZ235 NVP-BEZ235(BEZ235) - Reference Information
| Use | 2-methyl -2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)] -2, 3-dihydroimidazo [4,5-C] quinolin-1-yl] phenyl] Propionitrile is an inhibitor of phosphatidylinositol 3-kinase, P13K and mTOR, potent dual inhibitors of PI3K/mTOR. |
| biological activity | dacolisib (BEZ235, NVP-BEZ235) is a dual ATP competitive PI3K and mTOR inhibitor, in the cell-free assay, the IC50 for inhibition of p110α/γ/δ/β and mTOR(p70S6K) was 4 nM /5 nM /7 nM /75 nM /6 nM, respectively. ATR was inhibited in 3T3 pbp1-er cells with an IC50 of 21 nM, while Akt and PDK1 were weakly inhibited. Dactolisib induces autophagy and inhibits replication by HIV-1. Phase 2. |
| Target | Value |
| p110α (Cell-free assay) | 4 nM |
| p110γ (Cell-free assay) | 5 nM |
| mTOR (p70S6K) (Cell-free assay) | 6 nM |
| p110δ (Cell-free assay) | 7 nM |
| ATR (3T3 TopBP1-ER cells) | 21 nM |
Last Update：2024-04-09 02:00:12
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Spot supply
Product Name: NVP-BEZ 235 Visit Supplier Webpage Request for quotationCAS: 915019-65-7
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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