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evobrutinib

Name: evobrutinib
Brand: TargetMol
SKU: T4387
Price: 347 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.58%

货号 T4387Cas号 1415823-73-2

别名 MSC2364447C, M2951

Evobrutinib(M2951) 也称为 M-2951 和 MSC-2364447C，是布鲁顿酪氨酸激酶(BTK) 的高选择性抑制剂，BTK 对包括 B 淋巴细胞和巨噬细胞在内的各种免疫细胞的发育和功能很重要。临床前研究表明它可能对某些自身免疫性疾病有治疗作用。

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evobrutinib

一键复制产品信息

很棒

纯度: 99.58%

货号 T4387 别名 MSC2364447C, M2951Cas号 1415823-73-2

规格	价格	库存
1 mg	¥ 347	现货
5 mg	¥ 828	现货
10 mg	¥ 1,320	现货
25 mg	¥ 2,380	现货
50 mg	¥ 3,480	现货
100 mg	¥ 4,970	现货
200 mg	¥ 6,880	现货
1 mL x 10 mM (in DMSO)	¥ 892	现货

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产品介绍

evobrutinib AI Summary

evobrutinib exhibits potent inhibitory activity against various tyrosine kinases, notably BTK, TEC, BMX, and BLK, with inhibition percentages ranging from 42% to 90%. It demonstrates strong inhibition of BTK across different assays and cell types: an IC50 of 62.0 nM in full-length human recombinant BTK, 61.0 nM in human THP1 cells, 320.0 nM in human B cells, and 8.9 nM in N-terminal GST-fused human BTK, showing high binding affinity with a Kd of 16.0 nM. The compound also inhibits TEC, BMX, and ERBB4 with IC50 values of 37.9 nM, and shows low inhibition percentages (1%) on EGFR and ERBB2. Selectivity studies reveal higher affinity of evobrutinib for BTK relative to other kinases. Additionally, it demonstrates efficacy in various in vivo and in vitro models, including antiarthritic activity and the inhibition of GP6-mediated platelet aggregation. Despite its potent kinase inhibitory capabilities, evobrutinib shows modest activity against SARS-CoV-2, with low inhibition rates in viral protease and cytotoxicity assays. It exhibits oral bioavailability in animal models, a half-life in plasma, and favorable permeability across human Caco-2 cells. The compound is stable in plasma, maintaining 81.0% stability over 4 hours, and shows relatively high pharmacokinetic stability and favorable selectivity profiles in different experimental setups..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Evobrutinib(M2951) , also known as M-2951 and MSC-2364447C, is a highly selective inhibitor of the Bruton's tyrosine kinase (BTK), which is important in the development and functioning of various immune cells including B -lymphocytes and macrophages. PreClinical research suggests it may be therapeutically useful in certain autoimmune diseases.
靶点活性	BTK:37.9 nM
别名	MSC2364447C, M2951

化学信息

分子量	429.51
分子式	C₂₅H₂₇N₅O₂
CAS No.	1415823-73-2
Smiles	Nc1ncnc(NCC2CCN(CC2)C(=O)C=C)c1-c1ccc(Oc2ccccc2)cc1
密度	1.227 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 25 mg/mL (58.21 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.66 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3282 mL	11.6412 mL	23.2823 mL	116.4117 mL
5 mM	0.4656 mL	2.3282 mL	4.6565 mL	23.2823 mL
10 mM	0.2328 mL	1.1641 mL	2.3282 mL	11.6412 mL
20 mM	0.1164 mL	0.5821 mL	1.1641 mL	5.8206 mL
50 mM	0.0466 mL	0.2328 mL	0.4656 mL	2.3282 mL