SAR125884 hydrochlorid (1116743-46-4(free base)) NEW
| Price | $32 | $55 | $92 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: SAR125884 hydrochlorid (1116743-46-4(free base)) | Purity: 97.95% |
| Supply Ability: 10g | Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | SAR125884 hydrochlorid (1116743-46-4(free base)) |
| 描述 | SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM). |
| 動物實(shí)驗(yàn) | The antitumor activity of SAR125844 was investigated after administration of SAR125844 solution daily in SNU-5 bearing mice at 10, 20, and 45 mg/kg and every 2 days in Hs 746T tumor–bearing mice (at 5, 10, 20, and 45 mg/kg for SAR125844 solution and at 5, 11, 21, 53, 106, and 213 mg/kg for SAR125844 nanosuspension). Tumor volumes (in mm^3, based on the following formula, volume = length (mm) × width2 (mm2)/2), were measured twice weekly and body weight recorded every day. Endpoints collected were complete regressions (CR, regression below the palpable limit), partial regressions (PR, regression of 50% of the initial tumor volume), and the percentage of tumor regression (% of volume decrease posttreatment compared with pretreatment). Statistical significance was determined by a Dunnett test versus vehicle after a two-way ANOVA with repeated measures performed separately on ranks of changes from baseline with P < 0.05 considered significant[1]. |
| 體外活性 | MKN-45, Hs 746T, and SNU-5 cells were seeded in poly d-lysine 96-well plates in complete medium. Plates were incubated with increasing SAR125844 concentrations for 1 hour, cell lysates were generated using standard procedures and pMETY1230/1234/1235 level evaluated. IC50 values were calculated using the software and a 4-parameter logistic model[1]. |
| 體內(nèi)活性 | SAR125844 inhibited autophosphorylation of AXL and cell proliferation of TPM–NTRK1-overexpressing KM12 cell line with IC50 values of 110 and 1,400 nmol/L, respectively, indicating a 30- and 500-fold selectivity index for AXL and NTRK1 in cell-based assays. The selectivity profile of SAR125844 was further confirmed in cell lines with a single-digit nanomolar antiproliferative activity in MET-addicted cell lines and a complete lack of impact in cells not addicted to the MET pathway. This is in contrast to ARQ197 that has equal antiproliferative activity on MET-addicted and MET-independent tumor cell lines[1]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (93.7 mM) |
| 關(guān)鍵字 | SAR125884 hydrochlorid (1116743-46-4(free base)) | SAR-125884 hydrochlorid (1116743-46-4(free base)) | SAR125884 hydrochlorid (1116743464(free base)) | SAR125884 hydrochlorid (1116743 46 4(free base)) |
| 相關(guān)產(chǎn)品 | Cabozantinib | Capmatinib 2HCl | SGI-7079 | (±)-Norcantharidin | L-Ascorbic acid 2-phosphate trisodium | Crizotinib | Amuvatinib | Norcantharidin | Cabozantinib S-malate | Capmatinib xHCl | Bacitracin Zinc | Capmatinib |
| 相關(guān)庫 | 抗結(jié)直腸癌化合物庫 | 經(jīng)典已知活性庫 | 細(xì)胞因子抑制劑庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 | 激酶抑制劑庫 | 抑制劑庫 | 已知活性化合物庫 | 抗癌化合物庫 | 抗肝癌化合物庫 |
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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United States- Since: 2011-01-07
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