产品名称

英文名称：BEZ235

同义词

dactolisib、915019-65-7、NVP-BEZ235、BEZ235、NVP-BEZ 235、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、BEZ-235、NVPBEZ235、BEZ 235、NVP-BEZ-235、NVP BEZ235、BEZ235 (NVP-BEZ235)、RTB101、RTB-101、RUJ6Z

产品性质

CAS编号：915019-65-7

分子式：C30H23N5O

分子量：469.54

PubChem编号：11977753

英文别名：dactolisib|915019-65-7|NVP-BEZ235|BEZ235|NVP-BEZ 235|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|BEZ-235|NVPBEZ235|BEZ 235|NVP-BEZ-235|NVP BEZ235|BEZ235 (NVP-BEZ235)|RTB101|RTB-101|RUJ6Z

规格或纯度：≥99%

英文名称：BEZ235

生化机理：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 tumor cell lines in animal models of cancer. BEZ235 is an mTOR Complex 1 and mTOR Complex 2 catalytic inhibitor. BEZ235 also inhibits ATR (IC50 = 21nM).Potent, ATP-competitive Phosphatidylinositol 3- kinase\xa0(PI3K) inhibitor (IC 50 = 4, 5, 7 and 75 nM for PI3Kα, -γ, -δ, and -β respectively) and mTOR inhibitor. Able to directly induce G 1 arrest and inhibit angiogenesis in vitro and potentiate the effic

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：BEZ235 (NVP-BEZ235, Dactolisib) ATP竞争性的抑制PI3K和mTOR，对p110α/γ/δ/β和mTOR(p70S6K)均有抑制作用，IC50分别为4 nM/5 nM/7 nM/75 nM/6 nM，对ATR也有抑制作用，IC50为21 nM；但对Akt和PDK1抑制作用微弱。A dual PI3K and mTOR inhibitorBEZ235 (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.A dual PI3K and mTOR inhibitor

ALogP：5.2

IUPAC Name：2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile

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

CAS Registry No.：915019-65-7

Wikipedia：BEZ235

ChEMBL Ligand：CHEMBL1879463

Reactome Reaction：R-HSA-2400009

Reactome Drug：R-ALL-2399744

溶解性：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).

产品包装