型号:
产品价格:电议      采购度:1603      原产地:美洲
发布时间:2021/7/24 2:20:19 所属地区:上海 上海市
简要描述:
Dactolisib Tosylate (BEZ235 Tosylate) 是PI3K和mTOR的双重激酶抑制剂,对PI3Kα, β, γ, δ 的IC50值分别为4, 75, 7, 5 nM。Dactolisib Tosylate (BEZ235 Tosylate) 抑制 mTORC1 和 mTORC2。
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CAS No. : 1028385-32-1
MCE 站:Dactolisib Tosylate
产品活性:Dactolisib Tosylate (BEZ235 Tosylate) 是PI3K和mTOR的双重激酶抑制剂,对PI3Kα, β, γ, δ 的IC50值分别为4, 75, 7, 5 nM。Dactolisib Tosylate (BEZ235 Tosylate) 抑制 mTORC1 和 mTORC2。
研究领域:PI3K/Akt/mTOR | Autophagy
In Vitro: Dactolisib (BEZ235) is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. The IC50s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of Dactolisib (BEZ235), with an average GI50 of 10 to 12 nM.
In Vivo: Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, Dactolisib (BEZ235) appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Antioxidants Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Rapamycin | 3-Methyladenine | LY294002 | Wortmannin | Everolimus | MHY1485 | Quercetin | 740 Y-P | 3BDO | Temsirolimus | Salidroside | Torkinib | PI-103 | D-α-Hydroxyglutaric acid disodium | Isorhamnetin | L-Leucine | Recilisib | Autophinib | Dihydromyricetin | AZD 6482 | PI3K-IN-1 | TG100-115 | α-Linolenic acid | TGX-221 | 1-Deoxynojirimycin | YS-49 | AS-605240 | PKI-402 | Disitertide | Erucic acid
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更新时间:2024/1/2 10:14:29
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