Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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B126286-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $31.90 | |
B126286-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $103.90 | |
B126286-250mg | 250mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $234.90 | |
B126286-1g | 1g | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $842.90 |
Potent PI3K and mTOR inhibitor
Synonyms | BEZ235 | BEZ-235 | IRL-2500 is known as an ETB antagonist. | Lacidipinum | 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 | AMY2877 | CT-BEZ | HY-50673 | NVP-BEZ235 | NVP-BEZ-235 | SCHEMBL105 |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | BEZ235 is a PI 3-kinase (PI3K) tyrosine kinase inhibitor and shows dual PI3K/mTOR inhibition (IC50 = 4, 5, 7 and 75 nM for PI 3-Kα, -γ, -δ, and -β, respectively). BEZ235 showed high target specificity and demonstrated antiproliferative activity against tu |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | PI3-kinase class I inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM, respectively. Inhibits ATR with IC50 of 21 nM, whileshown to be a poor inhibitor to Akt and PDK1. |
ALogP | 5.2 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile |
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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 |
InChi Key | JOGKUKXHTYWRGZ-UHFFFAOYSA-N |
Canonical SMILES | CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5 |
Isomeric SMILES | CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5 |
PubChem CID | 11977753 |
Molecular Weight | 469.54 |
CAS Registry No. | 915019-65-7 |
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PubChem CID | 11977753 |
Wikipedia | BEZ235 |
ChEMBL Ligand | CHEMBL1879463 |
Reactome Reaction | R-HSA-2400009 |
Reactome Drug | R-ALL-2399744 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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A1523064 | Certificate of Analysis | Sep 13, 2022 | B126286 |
Solubility | Soluble in chloroform (1 mg/ml), 1-methyl-2-pyrrolidnone (2 mg/mL at 75 °C), DMSO (1.33 mg/mL), and DMF (10 mg/mL at 75 °C). |
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1. Dong Zhang, Jianglong Kong, Xueying Huang, Jie Zeng, Qiaohui Du, Tao Yang, Hui Yue, Qing Bao, Yao Miao, Yajing Xu, Honglin Jiang, Fang Lei, Mingying Yang, Yi Wang, Chuanbin Mao. (2023) Targeted Glioblastoma Therapy by Integrating Brain-Targeting Peptides and Corn-derived Cancer Cell-Penetrating Proteins into Nanoparticles to Cross Blood-Brain Tumor Barriers. Materials Today Nano, (100347). [PMID:] [10.1016/j.mtnano.2023.100347] |
1. Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K 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 (7): (1851-63). [PMID:18606717] [10.1021/op500134e] |
2. Willemsen-Seegers N, Uitdehaag JCM, Prinsen MBW, de Vetter JRF, de Man J, Sawa M, Kawase Y, Buijsman RC, Zaman GJR. (2017) Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance.. J Mol Biol, 429 (4): (574-586). [PMID:28043854] [10.1021/op500134e] |
3. Ma BB, Lui VW, Hui CW, Lau CP, Wong CH, Hui EP, Ng MH, Cheng SH, Tsao SW, Tsang CM et al.. (2014) Preclinical evaluation of the mTOR-PI3K inhibitor BEZ235 in nasopharyngeal cancer models.. Cancer Lett, 343 (1): (24-32). [PMID:24041865] [10.1021/op500134e] |
4. Fròsina G, Profumo A, Marubbi D, Marcello D, Ravetti JL, Daga A. (2018) ATR kinase inhibitors NVP-BEZ235 and AZD6738 effectively penetrate the brain after systemic administration.. Radiat Oncol, 13 (1): (76). [PMID:29685176] [10.1021/op500134e] |
5. Dong Zhang, Jianglong Kong, Xueying Huang, Jie Zeng, Qiaohui Du, Tao Yang, Hui Yue, Qing Bao, Yao Miao, Yajing Xu, Honglin Jiang, Fang Lei, Mingying Yang, Yi Wang, Chuanbin Mao. (2023) Targeted Glioblastoma Therapy by Integrating Brain-Targeting Peptides and Corn-derived Cancer Cell-Penetrating Proteins into Nanoparticles to Cross Blood-Brain Tumor Barriers. Materials Today Nano, (100347). [PMID:] [10.1016/j.mtnano.2023.100347] |