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MK-8033

MK-8033

产品编号 TQ0219   CAS 1001917-37-8

MK-8033 是一种新型ATP 竞争性c-Met/Ron 双重抑制剂,对野生型c-Met 的IC50=1 nM,对c-Met N1100Y 的IC50=2.0 nM。

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MK-8033 Chemical Structure
MK-8033, CAS 1001917-37-8
规格 价格/CNY 货期 数量
1 mg ¥ 1,170 现货
2 mg ¥ 1,730 现货
5 mg ¥ 2,490 现货
10 mg ¥ 3,770 现货
25 mg ¥ 6,070 现货
50 mg ¥ 8,370 现货
1 mL * 10 mM (in DMSO) ¥ 2,580 现货
其他形式的 MK-8033:
产品目录号及名称: MK-8033 (TQ0219)
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纯度: 97.16%
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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 MK-8033 is a new and selective dual ATP competitive c-Met/Ron inhibitor (IC50: 1 nM Wt c-Met).
靶点活性 c-Met (Wt):1 nM (cell free), c-Met (N1100Y):1 nM (cell free)
体外活性 MK-8033 binds 3-fold more tightly to phosphorylated c-Met kinase domain (Kd: 3.2 nM) than to its unphosphorylated counterpart (Kd = 10.4 nM). Significantly, MK-8033 potently inhibits the kinase activity of three oncogenic c-Met activation loop mutants, Y1230C, Y1230H, and Y1235D (IC50s: 0.6~1 nM at 50 uM ATP) in addition to other c-Met activating mutants N1100Y and M1250T. MK-8033 potently inhibited GTL-16 proliferation (IC50: 582 nM). By contrast, the HCT116 cell line, which does not harbor basal c-Met activation, was not inhibited by MK-8033 (IC50 > 10000 nM) [1]. MK-8033 radiosensitizer the high-c-Met-expressing EBC-1 and H1993 cells but not the low-c-Met-expressing cell lines A549 and H460. However, irradiation of A549 and H460 cells increased the expression of c-Met protein at 30 minutes after the irradiation. Subsequent targeting of this up-regulated c-Met by using MK-8033 followed by a second radiation dose reduced the clonogenic survival of both A549 and H460 cells. MK-8033reduced the levels of radiation-induced phosphorylated (activated) c-Met in A549 cells [2].
体内活性 MK-8033 was orally dosed in GTL-16 tumor xenograft bearing mice. Mice were euthanized 1 h after dosing and tested for p-Met (Y1349) in tumors and MK-8033 concentrations in plasma. At 100 mg/kg, essentially complete inhibition of p-Met (Y1349) was achieved. An in vivo IC50 of 1.3 uM was deduced from the relationship between plasma MK-8033 level and Met pY1349. Dosing at 3, 10, 30, and 100 mg/kg resulted in 22, 18, 57, and 86% tumor growth inhibition, respectively, relative to the tumor from vehicle-treated mice [1].
分子量 471.53
分子式 C25H21N5O3S
CAS No. 1001917-37-8

存储

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

溶解度

DMSO: 45 mg/mL (97.83 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1208 mL 10.6038 mL 21.2076 mL 53.0189 mL
5 mM 0.4242 mL 2.1208 mL 4.2415 mL 10.6038 mL
10 mM 0.2121 mL 1.0604 mL 2.1208 mL 5.3019 mL
20 mM 0.106 mL 0.5302 mL 1.0604 mL 2.6509 mL
50 mM 0.0424 mL 0.2121 mL 0.4242 mL 1.0604 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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参考文献

1. Northrup AB, et al, Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met. J Med Chem. 2013 Mar 28;56(6):2294-310. 2. Bhardwaj V, et al. C-Met inhibitor MK-8003 radiosensitizes c-Met-expressing non-small-cell lung cancer cells with radiation-induced c-Met-expression. J Thorac Oncol. 2012 Aug;7(8):1211-7.
Tepotinib BMS-754807 (±)-Norcantharidin BMS 777607 c-Met-IN-17 Merestinib Foretinib Norcantharidin

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 抗癌药物库 抗癌临床化合物库 抗癌活性化合物库 临床期小分子药物库 细胞重编程化合物库 ReFRAME 相关化合物库 抗肺癌化合物库 药物功能重定位化合物库 抗肝癌化合物库

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。
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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

MK-8033 1001917-37-8 Tyrosine Kinase/Adaptors c-Met/HGFR bladder cancer breast cancer EBC-1 H1993 MK 8033 anti-tumor Inhibitor GTL-16 radiosensitivity Anti-ancer MK8033 NSCLCs inhibit inhibitor

 

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