R406 free base NEW
| Price | $39 | $64 | $98 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: R406 free base | CAS No.: 841290-80-0 |
| Purity: 99.31% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | R406 free base |
| 描述 | R406 free base (R406 (free base)) is a potent Syk inhibitor. |
| 細(xì)胞實驗 | DLBCL cell lines are treated with serial dilutions of R406 (0.3, 0.6, 1.25, 2.5, or 5 μM) for 72 or 96 hours. Thereafter, cellular proliferation is determined by MTT assay, and cell apoptosis is assessed by using annexin V–FITC/propidium iodide (PI) staining. For the determination of caspase 9, 8, and 3, cells are lysed, size-fractionated by polyacrylamide gel electrophoresis (PAGE), and immunoblotted. (Only for Reference) |
| 激酶實驗 | In-vitro Fluorescence Polarization Kinase Assays: R406 is serially diluted in DMSO and then diluted to 1% DMSO in kinase buffer (20 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM MnCl2, 1 mM DTT, 0.1 mg/mL acetylated BGG). ATP and substrate in kinase buffer are added at room temperature, resulting in a final DMSO concentration on 0.2%. The kinase reactions are performed in a final volume of 20 μL containing 5 μM HS1 peptide substrate and 4 μM ATP and started by addition of 0.125 ng of Syk in kinase buffer. The reaction is allowed to proceed for 40 minutes at room temperature. The reaction is stopped by the addition of 20 μL of PTK quench mix containing EDTA/anti-phosphotyrosine antibody (1X final)/fluorescent phosphopeptide tracer (0.5X final) diluted in FP Dilution Buffer. The plate is incubated for 30 minutes in the dark at room temperature and then read on a Polarion fluorescence polarization plate reader. Data are converted to amount of phosphopeptide present using a calibration curve generated by competition with the phosphopeptide competitor provided in the Tyrosine Kinase Assay Kit. For IC50 determination, R406 is tested at eleven concentrations in duplicate and curve-fitting is performed by non-linear regression analysis using Prism GraphPad Software. |
| 體外活性 | Oral administration of R406 to mice with immune complex-induced inflammatory responses significantly inhibited the cutaneous reverse passive Arthus reaction, with treatments at 1 mg/kg and 5 mg/kg yielding suppression rates of 72% and 86% respectively, compared to the control group. Furthermore, treatment with 10 mg/kg R406 in mice pre-treated with collagen antibodies markedly reduced inflammation and swelling, diminished progressive arthritis to a lower level, and delayed the onset in the K/BxN serum transfer mouse model, reducing clinical arthritis severity by 50%. |
| 體內(nèi)活性 | Treatment with R406 at concentrations of 1 μM or 4 μM induces caspase 9 and 3 activation in DLBCL cell lines, leading to significant cell apoptosis without activating caspase 8. R406 selectively inhibits the Syk-dependent signaling pathways in various cells, demonstrating superior efficacy with EC50 values ranging from 33 nM to 171 nM compared to its effect on Syk-independent pathways. It effectively inhibits cell proliferation in diffuse large B-cell lymphoma (DLBCL) cell lines, with EC50 values between 0.8 μM to 8.1 μM. Pre-treatment with R406 completely blocks phosphorylation of SYK525/526 and SYK-dependent phosphorylation of BLNK post B-cell receptor (BCR) cross-linking in R406-sensitive DLBCL. Additionally, after 24 and 48 hours of R406 treatment, MMP-9 mRNA levels significantly reduced by 2.8 and 4.3 times, respectively, compared to control groups, thereby decreasing the invasiveness of RL cells. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 4.71 mg/mL (10 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| 關(guān)鍵字 | Inhibitor | FLT3 | Syk | Cluster of differentiation antigen 135 | R406 free base | inhibit | R-406 free base | CD135 | R406 | Fms like tyrosine kinase 3 | Apoptosis | Spleen tyrosine kinase | R 406 | R-406 |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
| 相關(guān)庫 | 細(xì)胞凋亡化合物庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 酪氨酸激酶分子庫 | 血管生成庫 | 抑制劑庫 | NO PAINS 化合物庫 | 已知活性化合物庫 | 含氟化合物庫 | 抗癌化合物庫 |
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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