Vevorisertib trihydrochloride NEW
| Price | $70 | $163 | $242 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-12 |
Product Details
| Product Name: Vevorisertib trihydrochloride | CAS No.: 1416775-08-0 |
| Purity: 98.28% | Supply Ability: 10g |
| Release date: 2024/11/12 |
Product Introduction
Bioactivity
| 名稱 | Vevorisertib trihydrochloride |
| 描述 | Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is a selective and potent inhibitor of pan-AKT and AKT1-E17K mutations, inhibiting AKT1, AKT2 and AKT3. Vevorisertib trihydrochloride is used in the study of hepatocellular carcinoma and advanced solid tumours. |
| 體外活性 | Vevorisertib trihydrochloride at concentrations ranging from 0 to 1000 nM over 2 hours inhibits the phosphorylation of AKT1-E17K. In NIH 3T3 cells transfected with pcDNAAKT-WT-GFP or pcDNA-E17K-GFP and treated with 1 μM of the compound for the same duration, it prevents the plasma membrane translocation of both AKT-WT and AKT1-E17K, regardless of growth factor presence. Additionally, a 5 μM concentration results in 57% inhibition of full-length AKT1. The compound demonstrates a dose-dependent impact on mTORC1 and AKT substrates, such as PRAS40, GSK3β, FOXO, BAD, and AS160 across various cancer cell lines with distinct concentrations (0 to 1 μM, 2 hours). It also exhibits significant anti-proliferative effects on esophageal, breast, and head and neck cancer cells, with GI 50 values below 1 μM, and showcases potent efficacy in PIK3CA mutant cell lines. Moreover, a combination of Vevorisertib trihydrochloride (MK-4440) and imatinib mesylate leads to cell cycle arrest and increased cell death in gastrointestinal stromal tumor cells. Western Blot analyses reveal the compound's effectiveness in inhibiting phosphorylation of AKT1-E17K and dose-dependent effects on mTORC1 and AKT substrates across different cell lines, including those with PIK3CA mutations and various cancer-related mutations. |
| 體內(nèi)活性 | Vevorisertib trihydrochloride administered orally at doses of 25, 50, and 75 mg/kg for five consecutive days followed by a four-day break over a 20-day period demonstrated significant tumor growth inhibition rates of 68%, 78%, and 98%, respectively, in endometrial PDX mouse xenograft models featuring the AKT1-E17K mutation. When administered daily at varying doses (5, 10, 20, 40, 80, and 120 mg/kg) for ten days in AN3CA mouse xenograft models, it showed tumor growth inhibition rates ranging from 29% to 92%. The compound achieved C max plasma concentrations of ≥2 μM and was generally well-tolerated at all administered doses up to 120 mg/kg. Additionally, a combination of Vevorisertib trihydrochloride (MK-4440) and IM exhibited superior efficacy in an IM-sensitive preclinical GIST model compared to either agent alone, highlighting its potential as a robust therapeutic candidate in specific cancer models. |
| 存儲條件 | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : 20 mg/mL (28.73 mM) DMSO : 100 mg/mL (143.66 mM), Sonication is recommended. |
| 關(guān)鍵字 | ARQ-751 Trihydrochloride | ARQ751 Trihydrochloride | ARQ751 | ARQ-751 | ARQ 751 | Vevorisertib | Vevorisertib trihydrochloride |
| 相關(guān)產(chǎn)品 | Ethyl gallate | Oridonin | Capivasertib | SKLB-163 | Scutellarin | Methyl-Hesperidin | Artemisinin | Honokiol | (E)-Akt inhibitor-IV | 2,3-Butanediol | MK-2206 dihydrochloride | AKT Kinase Inhibitor |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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