Gandotinib NEW
| Price | $47 | $80 | $163 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-01 |
Product Details
| Product Name: Gandotinib | CAS No.: 1229236-86-5 |
| Purity: 99.86% | Supply Ability: 10g |
| Release date: 2024/11/01 |
Product Introduction
Bioactivity
| 名稱(chēng) | Gandotinib |
| 描述 | LY2784544(Gandotinib (LY2784544)) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3. |
| 細(xì)胞實(shí)驗(yàn) | LY2784544 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Ba/F3 cells expressing JAK2V617F are placed in RPMI-1640-containing vehicle (DMSO) or LY2784544 (concentration range, 0.001-20 μM) (1×104 cells/96-well). Ba/F3 cells expressing wild-type JAK2 are treated similarly except IL-3 (2 ng/mL) is added. After a 72-hour incubation, cell proliferation is assessed by adding Cell Titer 96 Aqueous One Solution Reagent (20 μL/well). The IC50 for inhibition of cell proliferation is calculated using the GraphPad Prism 4 software[1]. |
| 體外活性 | In severe combined immunodeficient mice, LY2784544 (administered orally) does not affect CD71/Ter119 positive erythroid progenitor cells within the spleen. LY2784544 significantly inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts (effective dose 50% [ED50]: 12.7 mg/kg). Additionally, in a JAK2 V617F-induced myeloproliferative neoplasm (MPN) model, LY2784544 (administered orally) reduces the tumor burden of Ba/F3-JAK2 V617F-GFP (ED50: 13.7 mg/kg). |
| 體內(nèi)活性 | In proliferation assays, LY2784544 exhibits an anti-proliferative effect on JAK2 V617F-driven cells, with an IC50 of 68 nM. It demonstrates a less potent effect on cells driven by wild-type JAK2 and JAK3, with IC50 values of 1356 nM and 940 nM, respectively. LY2784544 also inhibits IL-3-activated wild-type JAK2 with an IC50 of 2.26 μM. |
| 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 : 87 mg/mL (185.1 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 9 mg/mL (19.15 mM) |
| 關(guān)鍵字 | LY-2784544 | VEGFR | inhibit | FGFR | LY 2784544 | Janus kinase | CD135 | FLT3 | Cluster of differentiation antigen 135 | Inhibitor | Fms like tyrosine kinase 3 | Vascular endothelial growth factor receptor | Gandotinib | JAK | Fibroblast growth factor receptor |
| 相關(guān)產(chǎn)品 | Ribociclib | Gilteritinib | Amlexanox | Nintedanib | Sorafenib | Tofacitinib Citrate | Ferulic Acid | Regorafenib | Ruxolitinib phosphate | Formononetin | Pazopanib | Axitinib |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 酪氨酸激酶分子庫(kù) | 激酶抑制劑庫(kù) | 抗癌臨床化合物庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌藥物庫(kù) | 抗癌活性化合物庫(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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United States- Since: 2011-01-07
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