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。
CAS No. : 934493-76-2
MCE 国际站:Voxtalisib
产品活性:Voxtalisib (XL765) 是一种有效的 PI3K 抑制剂,抑制p110α,p110β,p110γ 和 p110δ,IC50 分别为 39, 113, 9 和 43 nM,也抑制 DNA-PK (IC50=150 nM) 和 mTOR (IC50=157 nM)。Voxtalisib (XL765) 抑制 mTORC1 和 mTORC2,IC50s 分别为 160 和 910 nM。
研究领域:PI3K/Akt/mTOR
作用靶点:PI3K | mTOR
In Vitro: Voxtalisib (XL765) displays potent inhibitory activity against class I PI3K isoforms p110α, p110β, p110δ, and p120γ, with IC50s of 39, 110, 43, and 9 nM, respectively. The IC50 value for inhibition of PI3Kα by Voxtalisib is determined at various concentrations of ATP, revealing Voxtalisib be an ATP-competitive inhibitor with an equilibrium inhibition constant (Ki) value of 13 nM. Voxtalisib also inhibits mTOR (IC50s of 160 and 910 nM for mTORC1 and mTORC2, respectively) in an immune-complex kinase assay and the PI3K-related kinase DNA-PK (IC50 value of 150 nM). In contrast, Voxtalisib (XL765) has relatively weak inhibitory activity toward the class III PI3K vacuolar sorting protein 34 (VPS34; IC50 value of ~9.1 μM). Consistent with its inhibitory activity against purified PI3K proteins, SAR245409 inhibits EGF-induced PIP3 production in PC-3 and MCF7 cells with IC50s of 290 and 170 nM, respectively. The ability of Voxtalisib to inhibit phosphorylation of key signaling proteins downstream of PI3K is examined by assessing its effects on EGF-stimulated phosphorylation of AKT and on nonstimulated phosphorylation of S6 in PC-3 cells by cell-based ELISA. Voxtalisib inhibits these activities with IC50s of 250 and 120 nM, respectively. In MCF7 and PC-3 cells, Voxtalisib inhibits proliferation (monitored by BrdUrd incorporation) with IC50s of 1,070 and 1,840 nM, respectively. To further characterize the effects of Voxtalisib on tumor cell growth, an assay monitoring the anchorage-independent growth of PC-3 and MCF7 cells in soft agar over a 14-day period is used. SAR245409 inhibits colony growth with an IC50 value of 270 nM in PC-3 cells and 230 nM in MCF7 cells.
In Vivo: Oral administration of Voxtalisib (XL765) causes a dose-dependent decrease of phosphorylation of AKT, p70S6K, and S6 in the tumors, reaching a maximum of 84% inhibition of S6 phosphorylation at 30 mg/kg at 4 hours. The dose-response relationships derive from the 4 hours time point predict 50% inhibition of AKT, p70S6K, and S6 phosphorylation to occur at doses of 19 mg/kg (pAKTT308 and pAKTS473), 51 mg/kg (p-p70S6K), and 18 mg/kg (pS6). Inhibition of AKT, p70S6K, and S6 phosphorylation in MCF7 tumors following a 30 mg/kg dose of Voxtalisib is maximal at 4 hours, reaching 61% to 84%; however, the level of inhibition decreases to 0% to 42% by 24 hours, and minimal or no inhibition is evident by 48 hours. Following a 100 mg/kg dose of Voxtalisib, inhibition is also maximal at 4 hours (52%-75%).
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 | Anti-COVID-19 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。