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
- Molecular Weight:
- 469.55
- MDL Number:
- MFCD10565944
- MOL File:
- 915019-65-7.mol
- MSDS File:
- SDS
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 |
FDA UNII | RUJ6Z9Y0DT |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302 | |||||||||
Precautionary statements | P280-P305+P351+P338 | |||||||||
NFPA 704 |
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NVP-BEZ 235 price More Price(37)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 10565 | NVP-BEZ235 ≥98% | 915019-65-7 | 25mg | $44 | 2024-03-01 | Buy |
Cayman Chemical | 10565 | NVP-BEZ235 ≥98% | 915019-65-7 | 50mg | $78 | 2024-03-01 | Buy |
Cayman Chemical | 10565 | NVP-BEZ235 ≥98% | 915019-65-7 | 100mg | $138 | 2024-03-01 | Buy |
Cayman Chemical | 10565 | NVP-BEZ235 ≥98% | 915019-65-7 | 250mg | $235 | 2024-03-01 | Buy |
Usbiological | 018621 | NVP-BEZ 235 | 915019-65-7 | 10mg | $375 | 2021-12-16 | Buy |
NVP-BEZ 235 Chemical Properties,Uses,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
Inhibitor of phosphatidylinositol 3-kinases, P13K and mTOR.
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
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.
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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Capot Chemical Co.,Ltd. | +86-(0)57185586718 +86-13336195806 | sales@capot.com | China | 29791 | 60 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21634 | 55 |
Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 | product@chemlin.com.cn | CHINA | 3009 | 60 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32957 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29880 | 58 |
Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 965 | 58 |
Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22963 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | sales@chemdad.com | China | 39894 | 58 |
Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63687 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49374 | 58 |
View Lastest Price from NVP-BEZ 235 manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2024-11-19 | Dactolisib
915019-65-7
|
US $52.00-108.00 / mg | 99.85% | 10g | TargetMol Chemicals Inc. | |||
2021-07-02 | NVP-BEZ 235
915019-65-7
|
US $15.00-10.00 / KG | 1KG | 99%+ HPLC | Monthly supply of 1 ton | Zhuozhou Wenxi import and Export Co., Ltd | ||
2019-07-06 | NVP-BEZ 235
915019-65-7
|
US $1.00 / KG | 1G | 98% | 100KG | Career Henan Chemical Co |
- Dactolisib
915019-65-7
- US $52.00-108.00 / mg
- 99.85%
- TargetMol Chemicals Inc.
- NVP-BEZ 235
915019-65-7
- US $15.00-10.00 / KG
- 99%+ HPLC
- Zhuozhou Wenxi import and Export Co., Ltd
- NVP-BEZ 235
915019-65-7
- US $1.00 / KG
- 98%
- Career Henan Chemical Co