Epacadostat NEW
Price | $39 | $64 | $89 |
Package | 5mg | 10mg | 25mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-17 |
Product Details
Product Name: Epacadostat | CAS No.: 1204669-58-8 |
Purity: 99.93% | Supply Ability: 10g |
Release date: 2024/11/17 |
Product Introduction
Bioactivity
名稱 | Epacadostat |
描述 | Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM. |
細(xì)胞實(shí)驗(yàn) | INCB 024360 (INCB024360) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. To determine INCB 024360 activity against IDO in recombinant cells, HEK293/MSR cells are transiently transfected with full-length human or mouse IDO1, or mouse IDO2 cDNA, with Transit-293 transfection reagent or Lipofectamine 2000 reagents. INCB 024360 at different concentrations is added to the recovered transfected cells seeded at 2×104 cells per well in a 96-well plate (200 μL/well). The cells are incubated for 2 days, and kyn in the supernatants is measured as described in the HeLa cell assay. The tryptophan 2,3-dioxygenase (TDO) assay is performed similarly with HEK293/MSR cells transfected with a human TDO expression vector[1]. |
體外活性 | METHODS: Epacadostat (INCB 024360) (0.0001, 0.01, 1, 100, 10000nM) was used to treat SKOV-3 cells and the release of kynurenine was measured. RESULTS Epacadostat (INCB 024360) inhibited the catalytic activity of IDO1 with an IC50 value of 17.63 nM ± 2.26 (pIC50 = 7.76 ± 0.06). [2] |
體內(nèi)活性 | METHODS: Mice were injected subcutaneously with 200 μl TC-1 cells on the back. After the tumor was palpable, Epacadostat (INCB 024360) (50 mg/kg), IFN-γ (100 ng/mouse), and kynurenine (100 mg/kg) were injected intraperitoneally every day. Tumor volume was measured every 3 days. RESULTS Intraperitoneal injection of Epacadostat (INCB 024360) caused a significant increase in tumor volume and tumor weight, and inhibited the expression of CD80 on macrophages in tumor tissues. [3] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : 53 mg/mL (120.94 mM) DMSO : 50 mg/mL (114.1 mM) |
關(guān)鍵字 | inhibit | INCB024360 | INCB-024360 | Inhibitor | Epacadostat | Indoleamine 2,3-Dioxygenase (IDO) |
相關(guān)產(chǎn)品 | Palmatine chloride | GNF-PF-3777 | Coptisine chloride | Necrostatin-1 | IDO-IN-7 | Indoximod | Palmatine | β-Lapachone | IDO-IN-12 |
相關(guān)庫 | 表型篩選靶點(diǎn)鑒定庫 | 經(jīng)典已知活性庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 臨床期小分子藥物庫 | 已知活性化合物庫 | 抗癌化合物庫 | 抗癌藥物庫 | 抗癌活性化合物庫 |
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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