Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (97.83 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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