Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MS4078 是一种基于 Cereblon 配体的间变性淋巴瘤激酶 PROTAC ,结合 ALK 的 Kd 为 19 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 372 | 现货 | ||
2 mg | ¥ 542 | 现货 | ||
5 mg | ¥ 892 | 现货 | ||
10 mg | ¥ 1,380 | 现货 | ||
25 mg | ¥ 2,550 | 现货 | ||
50 mg | ¥ 3,930 | 现货 | ||
100 mg | ¥ 5,490 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,180 | 现货 |
产品描述 | MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK. |
靶点活性 | NPM-ALK:11 nM(DC50)(SU-DHL-1 cells), ALK:33 nM(SU-DHL-1 cells), EML4-ALK:59 nM(DC50)(NCI-H2228 cells) |
体外活性 | MS4078 effectively inhibits cancer cell proliferation. MS4078 induces ALK protein degradation via cereblon and proteasome dependent mechanism and potently inhibits proliferation of SU-DHL-1?cells with IC50 of 33 nM. MS4078 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228?cells in a concentration-dependent manner. MS4078 reduces the NPM-ALK protein levels in SU-DHL-1 cells and the EML4-ALK protein levels in NCI-H2228 cells with DC50 of 11 nM and 59 nM, respectively. |
分子量 | 914.47 |
分子式 | C45H52ClN9O8S |
CAS No. | 2229036-62-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 49 mg/mL (53.58 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.0935 mL | 5.4676 mL | 10.9353 mL | 27.3382 mL |
5 mM | 0.2187 mL | 1.0935 mL | 2.1871 mL | 5.4676 mL | |
10 mM | 0.1094 mL | 0.5468 mL | 1.0935 mL | 2.7338 mL | |
20 mM | 0.0547 mL | 0.2734 mL | 0.5468 mL | 1.3669 mL | |
50 mM | 0.0219 mL | 0.1094 mL | 0.2187 mL | 0.5468 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。
MS4078 2229036-62-6 Angiogenesis PROTAC Tyrosine Kinase/Adaptors ALK Ligand for E3 Ligase Anaplastic lymphoma kinase CD246 Inhibitor MS 4078 ALK tyrosine kinase receptor inhibit MS-4078 Anaplastic lymphoma kinase (ALK) PROTACs Cluster of differentiation 246 inhibitor