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Merestinib

Merestinib

产品编号 T3455   CAS 1206799-15-6
别名: LY2801653

Merestinib (LY2801653) 是一种有效的口服生物可利用的具有抗肿瘤活性的c-Met 抑制剂。

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Merestinib Chemical Structure
Merestinib, CAS 1206799-15-6
规格 价格/CNY 货期 数量
1 mg ¥ 336 现货
2 mg ¥ 475 现货
5 mg ¥ 747 现货
10 mg ¥ 1,230 现货
25 mg ¥ 2,370 现货
50 mg ¥ 3,530 现货
100 mg ¥ 4,970 现货
500 mg ¥ 10,700 现货
1 mL * 10 mM (in DMSO) ¥ 822 现货
其他形式的 Merestinib:
产品目录号及名称: Merestinib (T3455)
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纯度: 99.56%
纯度: 95%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Merestinib (LY2801653) is an orally available, small molecule inhibitor of the proto-oncogene c-Met (Ki: 2 nM) with potential antineoplastic activity. Merestinib electively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing the constitutively activated c-Met protein.
靶点活性 Met:2 nM(Ki)
体外活性 LY2801653 demonstrates in vitro effects on MET pathway-dependent cell scattering and cell proliferation. It demonstrates more potent anti-proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) than the cell lines without MET gene amplification (U-87 mg, KATO-III). LY2801653 also maintains potency against 13 MET variants, each bearing a single-point mutation. It is found to have potent activity against several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2 and against the serine/threonine kinases MKNK1/2. The mean IC50 value of LY2801653 for inhibition of MET auto-phosphorylation in HGF-stimulated H460 cells is 35.2±6.9 nM and the IC50 for MET auto-phosphorylation in S114 cells is 59.2 nM[1].
体内活性 LY2801653 shows in vivo anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87 mg, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects. It is able to induce vessel normalization in xenograft tumors. Among the species studied, LY2801653 has the shortest elimination half life in mice of 2.9 h, compared with 14.3 h in non-human primate. LY2801653 is currently in phase 1 Clinicalal testing in patients with advanced cancer[1].
激酶实验 The Ki value and mode of inhibition of LY2801653 for the MET kinase activity are determined using a radiometric filter-binding assay. Reactions are carried out in 96-well plates in Enzyme dilution buffer (EDB) compose of 50 mM Tris HCl pH 7.5, 2 mM DTT, 0.005% Triton X-100, 10 mM MgCl2, and 250 ?M EDTA. Serially diluted LY2801653 (final concentration 250 to 0 nM) are followed by the addition of a series of 8 concentrations of 33P-γ-ATP (final concentration 400 to 10 μM ATP), and 5 nM enzyme (final concentration). After a 2-hour incubation, PolyGluTyr synthetic protein substrate (final 150 μg/mL) is added to initiate the 30-minute kinase reaction. Reactions are quenched with 10% H3PO4, transfer to a pre-wetted Multiscreen anionic phosphocellulose 96-well filter plate, and washed; radioactivity is measured with a scintillation counter. The experimental data are fit to a global mix model inhibition equation using GraphPad Prism softwar to generate an alpha value to determine the modality of inhibition and to calculate the Ki value for LY2801653[1].
细胞实验 2×103 DU145 cells/well on poly-D-lysine 96-well black/clear plates are treated with LY2801653 (in 0.4 % DMSO), immediately followed by the addition of human HGF (20 ng/ml), and incubated for 48 h at 37 °C. 2 % formaldehyde fixed cells are stained with AlexaFluor 488 Phalloidin and counterstained with Propidium Iodide. Colony counts are quantified on Acumen Explorer? laser-scanning fluorescence microplate cytometer. A colony is defined as≥4 cells.(Only for Reference)
别名 LY2801653
分子量 552.53
分子式 C30H22F2N6O3
CAS No. 1206799-15-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 93 mg/mL (168.3 mM)

DMSO: 93 mg/mL (168.3 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.8099 mL 9.0493 mL 18.0986 mL 45.2464 mL
5 mM 0.362 mL 1.8099 mL 3.6197 mL 9.0493 mL
10 mM 0.181 mL 0.9049 mL 1.8099 mL 4.5246 mL
20 mM 0.0905 mL 0.4525 mL 0.9049 mL 2.2623 mL
50 mM 0.0362 mL 0.181 mL 0.362 mL 0.9049 mL
100 mM 0.0181 mL 0.0905 mL 0.181 mL 0.4525 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Yan SB, et al. Invest New Drugs. 2013, 31(4):833-44.
AEE788 VX-11e Edicotinib JI6 UNC2541 SB1317 hydrochloride (1204918-72-8(free base)) 7BIO PF-03814735

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 NO PAINS 化合物库 临床期小分子药物库 铜死亡化合物库 抗癌化合物库 药物功能重定位化合物库 细胞重编程化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Merestinib 1206799-15-6 Angiogenesis Immunology/Inflammation Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) FLT c-Met/HGFR ROS ROS Kinase LY-2801653 Discoidin Domain Receptor inhibit CD135 Fms like tyrosine kinase 3 FLT3 LY 2801653 Inhibitor LY2801653 Cluster of differentiation antigen 135 inhibitor

 

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