Evobrutinib
别名: M-2951, MSC-2364447C
Evobrutinib是一种高度选择性的BTK抑制剂，IC50为37.9 nM，具有潜在的抗肿瘤活性。
Evobrutinib Chemical Structure
CAS: 1415823-73-2
产品质控
Evobrutinib相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| Sf21 | Function assay | 1 uM | Inhibition of N-terminal His6-tagged full length human BMX expressed in Sf21 cells at 1 uM | 31368705 | |
| Sf21 | Function assay | 1 uM | Inhibition of N-terminal His6-tagged human TEC (174 to end aminoacids) expressed in baculovirus infected Sf21 cells at 1 uM | 31368705 | |
| THP1 | Function assay | 24 hrs | Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by HTRF assay, IC50=0.061μM | 32083858 | |
| PBMC | Function assay | 60 mins | Inhibition of BTK in human PBMC cells assessed as reduction in anti-IgM-stimulated CD69 expression on B cells preincubated for 60 mins followed by goat F(ab')2 anti-human IgM stimulation and measured after overnight incubation by flow cytometry, IC50=0.061μM | 31368705 | |
| B cells | Function assay | 60 mins | Inhibition of BTK in human B cells assessed as reduction in anti-IgM/IL4-stimulated CD69 expression on B cells preincubated for 60 mins followed by anti-IgM antibody/IL4 stimulation and measured after 16 hrs by flow cytometry, IC50=0.32μM | 32083858 | |
| HEK293 | Function assay | Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by HPLC analysis, Ki=3.1μM | 31368705 | ||
| Sf21 | Function assay | Inhibition of N-terminal GST-tagged human EGFR (696 to end aminoacids) expressed in baculovirus infected Sf21 cells, IC50=5.8μM | 31368705 | ||
| BTI-TN-5B1-4 | Function assay | Covalent binding affinity to human BTK (382 to 659 residues) expressed in baculovirus infected BTI-TN-5B1-4 insect cells by isothermal calorimetry | 31368705 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Evobrutinib是一种高度选择性的BTK抑制剂，IC50为37.9 nM，具有潜在的抗肿瘤活性。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Evobrutinib能抑制BTK的活性，阻止BCR信号通路的激活。它可通过羟基化、水解作用、O-去烷基化、葡萄苷酸化和谷胱甘肽结合代谢[2]。 |
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|---|---|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05248945 | Completed | Healthy |
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany |
January 13 2022 | Phase 1 |
| NCT04546789 | Completed | Hepatic Impairment |
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany |
September 30 2020 | Phase 1 |
| NCT04314024 | Completed | Healthy |
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany |
May 25 2020 | Phase 1 |
| NCT03934502 | Completed | Healthy |
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany |
April 15 2019 | Phase 1 |
化学信息&溶解度
| 分子量 | 429.51 | 分子式 | C25H27N5O2 |
| CAS号 | 1415823-73-2 | SDF | -- |
| Smiles | C=CC(=O)N1CCC(CC1)CNC2=NC=NC(=C2C3=CC=C(C=C3)OC4=CC=CC=C4)N | ||
| 储存条件(自收到货起) | 3年 -20°C 粉状 | ||
|
体外溶解度 |
DMSO : 86 mg/mL ( (200.22 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 10 mg/mL (23.28 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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