Product Details
| Product Name:
MLN9708 |
CAS No.:
1201902-80-8 |
| Purity:
≥95% |
Supply Ability:
10g |
| Release date:
2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | MLN9708 |
| 描述 | MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma. |
| 細(xì)胞實(shí)驗(yàn) | Calu-6 cells are cultured in MEM containing 10% FBS and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentrations of Bortezomib or MLN2238 in DMSO (0.5% final, v/v) for 1 hour at 37 °C. For reversibility experiments, cells are treated with either 1 μM Bortezomib or MLN2238 for 30 minutes at 37 °C and then washed thrice in medium to remove the Bortezomib or MLN2238. Cells are incubated for an additional 4 hours at 37 °C, after which the medium is removed and replaced with fresh medium. (Only for Reference) |
| 激酶實(shí)驗(yàn) | Kinase assay: Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents according to the manufacturer's instructions. Luminescence is measured using a LEADseeker instrument. |
| 體外活性 | MLN9708 exhibits anticancer activity in a variety of solid tumors and hematologic malignancies. |
| 體內(nèi)活性 | Upon contact with aqueous solutions and plasma, MLN9708 rapidly hydrolyzes into MLN2238, which possesses bioactivity. MLN2238 inhibits the chymotrypsin-like hydrolytic sites of the 20S proteasome ([IC50=3.4 nM,Ki=0.93 nM]). It also inhibits the caspase-like ([IC50=31 nM]) and trypsin-like hydrolytic sites ([IC50=3.5 μM]) of the 20S proteasome. |
| 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 | DMSO : 93 mg/mL (179.8 mM)
|
| 關(guān)鍵字 | MLN 9708 | MLN-9708 | MLN9708 |
| 相關(guān)產(chǎn)品 | Sitagliptin | Teneligliptin hydrobromide | Sitagliptin phosphate monohydrate | Anagliptin | TCH-165 | Racecadotril | Linagliptin | Aprotinin | Vildagliptin | Alloxan monohydrate | 4'-Hydroxychalcone | Bortezomib |
| 相關(guān)庫 | FDA上市及藥典收錄分子庫 | 經(jīng)典已知活性庫 | 蛋白酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抗癌上市藥物庫 | FDA 上市藥物庫 | 已知活性化合物庫 | 抗癌活性化合物庫 | 抗癌藥物庫 |
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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