NVP-BEZ 235
- Product Name
- NVP-BEZ 235
- CAS No.
- 915019-65-7
- Chemical Name
- NVP-BEZ 235
- Synonyms
- 104794;CS-381;BEZ-235;Dactolisib;NVP-BEZ 235;BEZ235 0.6G;BEZ235, >=98%;NVP-BEZ235(BEZ235);BEZ235 (NVP-BEZ235);Dactolisib (BEZ235)
- CBNumber
- CB01872365
- Molecular Formula
- C30H23N5O
- Formula Weight
- 469.55
- MOL File
- 915019-65-7.mol
NVP-BEZ 235 Property
- Melting point:
- 288-289°C
- Boiling point:
- 701.0±70.0 °C(Predicted)
- Density
- 1.299
- storage temp.
- Refrigerator
- solubility
- Soluble in DMSO (up to 1 mg/ml with warming) or in DMF (up to 10 mg/ml, dissolves slowly, requires heating to 75?C).
- pka
- 6.41±0.20(Predicted)
- form
- White powder.
- color
- White or off-white
- 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.
- CAS DataBase Reference
- 915019-65-7
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 10565
- Product name
- NVP-BEZ235
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 10565
- Product name
- NVP-BEZ235
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $78
- Updated
- 2024/03/01
- Product number
- 10565
- Product name
- NVP-BEZ235
- Purity
- ≥98%
- Packaging
- 100mg
- Price
- $138
- Updated
- 2024/03/01
- Product number
- 10565
- Product name
- NVP-BEZ235
- Purity
- ≥98%
- Packaging
- 250mg
- Price
- $235
- Updated
- 2024/03/01
- Product number
- N925750
- Product name
- NVP-BEZ235
- Packaging
- 10mg
- Price
- $45
- Updated
- 2021/12/16
NVP-BEZ 235 Chemical Properties,Usage,Production
Description
NVP-BEZ235 (915019-65-7) is a dual PI3K and mTOR kinase inhibitor.1?It inhibits VEGF-induced proliferation and angiogenesis.2?Reverses lapatinib resistance.3?It induces G1 arrest and reduces cyclin D1 expression in melanoma cells with negligible apoptosis.4?NVP-BEZ235 inhibits the growth of cancer cells with activating PI3K mutations.5?The ability of NVP-BEZ235 to inhibit PI3K has come into question. This study also shows it to be a potent inhibitor of PRKDC (IC50 = 29 nM), ATM (IC50 = 13 nM), and ATR (IC50 = 8 nM).6?Active in vivo.
Chemical Properties
Light Beige Solid
Uses
A dual ATP-competitive inhibitor of PI3K and mTOR. p110α, IC50=4 nM; p110β, IC50=75 nM; p110δ, IC50=7 nM; p110γ, IC50=5 nM.
Uses
Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of PI3K and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies. It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase. Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis. By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.[Cayman Chemical]
Uses
Inhibitor of phosphatidylinositol 3-kinases, P13K and mTOR.
Definition
ChEBI: An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.
in vivo
BEZ235 induced tumor regression (69%) without a statistically significant effect on weight gain. Taken together, these preliminary in vivo efficacy findings suggest that BEZ235 blocks disease progression when administered orally alone and enhances efficacy when combined with other anticancer drugs.
target
p110α
References
1) Maira et al. (2008), 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., 7 1851 2) Schnell et al. (2008), Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging; Cancer Res., 68 6598 3) Eichhorn et al. (2008), Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/Phosphatidylinositol 3-kinase inhibitor NVP-BEZ235; Cancer Res., 68 9221 4) Marone et al. (2009), Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors; Mol. Cancer Res., 7 601 5) Serra et al. (2008), NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations; Cancer Res., 68 8022 6) Reinecke?et al. (2019),?Chemoproteomic selectivity profiling of PIKK and PI3K kinase inhibitors; ACS Chem.Biol., 14?655
NVP-BEZ 235 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from NVP-BEZ 235 manufacturers
- Product
- NVP-BEZ 235 915019-65-7
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-06-27
- Product
- NVP-BEZ 235 915019-65-7
- Price
- US $1.00/KG
- Min. Order
- 1G
- Purity
- 98%
- Supply Ability
- 100KG
- Release date
- 2018-08-21