MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Dactolisib Tosylate

CAS No. : 1028385-32-1

MCE 国际站：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

作用靶点：PI3K  |  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 PI3Kα^E545K or PI3Kα^H1047R 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 C_max of 1.68 μM at 0.5 h and a C_24h 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  |  Antioxidant 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  |  Anti-Cancer Metabolism Compound Library  |  Anti-Obesity Compound Library  |  Angiogenesis-Related Compound Library  |  Lipid Metabolism Compound Library   |  Glucose Metabolism Compound Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Human Metabolite Library  |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Cancer Stem Cells Compound Library  |  Pain-Related Compound Library  |  Mitochondrial Protection Compound Library  |  Membrane Protein-targeted Compound Library  |  D-α-Hydroxyglutaric acid disodium  |  Umbralisib hydrochloride  |  PI3K-IN-22  |  Rigosertib sodium  |  PI3Kδ/γ-IN-2  |  PI3kδ inhibitor 1  |  WYE-354  |  GSK2292767  |  PI3K-IN-28  |  PI3K/mTOR Inhibitor-13  |  Disitertide diammonium  |  1,3-Dicaffeoylquinic acid  |  Palomid 529  |  Quercetin dihydrate  |  PI3Kγ inhibitor 4  |  PI-103 Hydrochloride  |  Hirsutenone  |  SN32976  |  (+)-Usnic acid  |  Sophocarpine monohydrate  |  Heterophyllin B  |  IC-87114  |  Phosphatidylinositol 4,5-bisphosphate  |  Chaetominine  |  SF2523  |  Flupentixol  |  8-Aminoadenosine  |  GNE-490  |  MHY-1685  |  AZD-7648

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。