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- 2026年07月07日
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- 文献和实验
- 技术资料
- CAS号：
1116743-46-4
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥268.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥706.0 |
| 规格： | 5mg | 产品价格： | ￥596.0 |
| 规格： | 10mg | 产品价格： | ￥944.0 |
| 规格： | 25mg | 产品价格： | ￥1904.0 |
| 规格： | 50mg | 产品价格： | ￥3080.0 |
| 规格： | 100mg | 产品价格： | ￥4392.0 |
| 规格： | 200mg | 产品价格： | ￥5984.0 |
Product Introduction
Bioactivity
| 名称 | SAR125844 |
| 描述 | SAR125844, a potent and highly selective inhibitor of the MET receptor tyrosine kinase (RTK), for intravenous administration. (IC50 value of 4.2 nmol/L) |
| 细胞实验 | 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 Biost@t-SPEED internal software and a 4-parameter logistic model |
| 激酶实验 | SAR125844 was preincubated at room temperature with each enzyme for 30 minutes in a buffer containing 10 mmol/L MOPS-NaOH pH 7.0, 0.01% Tween 20, and 1 mmol/L dithiothreitol. The enzymatic reactions were initiated by the addition of a mix of 1 ng/μL of a biotinylated poly(glutamate-alanine-tyrosine) peptide ATP and MgCl2. After 5-minute incubation at room temperature, the reactions were stopped by the addition of anti-phosphotyrosine monoclonal antibody (mAb) PT-66 -Europium cryptate and streptavidin 61SAXLB. After two hours at room temperature, the emission signals at 620 and 665 nm were recorded with a GENios reader, with an excitation wavelength of 320 nm. The percentage of inhibition versus nontreated sample was estimated using the emission ratios at 665/620 nm. |
| 动物实验 | Long duration of MET kinase inhibition up to 7 days was achieved with a nanosuspension formulation of SAR125844.?Daily or every-2-days intravenous treatment of SAR125844 promoted a dose-dependent tumor regression in MET-amplified human gastric cancer models at tolerated doses without treatment-related body weight loss. |
| 体外活性 | SAR125844在纳摩尔范围内，通过细胞实验抑制MET自磷酸化作用，并且在具有MET基因扩增或路径依赖的细胞系中，以低纳摩尔浓度选择性促进凋亡和抗增殖活性。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 45 mg/mL (81.72 mM), Sonication is recommended. 10% DMSO+90% Corn Oil : 2 mg/mL (3.63 mM), Sonication is recommended. |
| 关键字 | SAR-125884 | SAR-125844 | SAR125844 | SAR 125884 | SAR 125844 | MET RTK | Inhibitor | inhibit | HGFR | c-Met/HGFR | cMet/HGFR | c-Met | cMet | Apoptosis |
| 相关产品 | Formamide | Urea | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen | Ethyl linoleate |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Highly Selective Inhibitor Library | Immunology/Inflammation Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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相关实验
网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 SAR125844【1116743-46-4】
￥268 - 5984
