Dactolisib Tosylate NEW
Price | $42 | $59 |
Package | 25mg | 50mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-01 |
Product Details
Product Name: Dactolisib Tosylate | CAS No.: 1028385-32-1 |
Purity: 99.85% | Supply Ability: 10g |
Release date: 2024/11/01 |
Product Introduction
Bioactivity
名稱 | Dactolisib Tosylate |
描述 | Dactolisib Tosylate (BEZ235 Tosylate) is a dual kinase inhibitor targeting PI3K and mTOR, with IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. It also inhibits mTORC1 and mTORC2. |
體外活性 | Dactolisib (BEZ235) exhibits IC50 values of 4 nM, 75 nM, 7 nM, and 5 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Furthermore, it demonstrates significant activity against mutant forms of PI3Kα, specifically PI3KαE545K and PI3KαH1047R, with IC50 values of 5.7 nM and 4.6 nM, respectively. Treatment with increasing concentrations of Dactolisib (BEZ235) leads to a dose-dependent reduction in cell proliferation in PTEN-null cell lines PC3M and U87MG, with an average GI50 ranging from 10 to 12 nM. Notably, in human tumor cell lines, it effectively and specifically blocks the aberrant activation of the PI3K pathway, leading to G1 arrest.[1] |
體內(nèi)活性 | Dactolisib (BEZ235) (50 mg/kg) appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM. BEZ235 is well tolerated, and displays disease stasis when administered orally. It enhances the efficacy of other anticancer agents.[1] |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : 0.1 mg/mL (insoluble) DMSO : 30.6 mg/mL (47.7 mM), Sonication and heating are recommended. |
關(guān)鍵字 | BEZ-235 Tosylate | Dactolisib Tosylate | BEZ 235 Tosylate | NVP-BEZ235 Tosylate | NVP-BEZ-235 Tosylate |
相關(guān)產(chǎn)品 | L-Leucine | Myricetin | Erucic acid | Sapanisertib | Isoprenaline hydrochloride | Quercetin | Quercetin Dihydrate | Rapamycin | Apilimod |
相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 臨床期小分子藥物庫(kù) | 已知活性化合物庫(kù) | 抗癌化合物庫(kù) | 抗癌藥物庫(kù) |
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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- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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