|4-(叔丁基)-N-(2-甲基-3-(4-甲基-6-((4-(吗啉-4-羰基)苯基)氨基)-5-氧代-4,5-二氢吡嗪-2-基)苯基)苯甲酰胺|CsnPharm

CAS No.: 910232-84-7

CGI-1746 Catalog No. CSN13815

Synonyms: CGI-1746

CGI-1746 is a Bruton's tyrosine kinase (Btk) inhibitor.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Bruton's tyrosine kinase (BTK) is a non-receptor tyrosine kinase that plays a critical role in development, differentiation and proliferation of B-lineage cells. CGI-1746 is an ATP-competitive small molecule inhibitor of BTK with IC₅₀ value of 1.9 nM. In vitro, CGI-1746 potently inhibited all three anti-IgM-induced phosphorylation events in both human and murine B cells with an average IC₅₀ value of 2.9 nM, and completely inhibited the proliferation of CD27⁺IgG⁺ B cells, anti-IgM-induced murine and human B cell, with IC₅₀ values of 112 nM, 134 nM and 42 nM, respectively. However, CGI1746 had no effect on anti-CD3 and anti-CD28 induced T cell proliferation^[3]. CGI1746 could also inhibit the growth of human myeloma cell line APR1 and OCI-MY5 with IC₅₀ value of 10 μM^[4]. CGI1746 decreases cytokine levels within joints and ameliorates disease in myeloid- and FcgR-dependent autoantibody-induced arthritis. In vivo, administration of 100 mg/kg twice-daily with CGI-1746 for 4 weeks significantly inhibited overall clinical arthritis scores, and reduced anti-collagen II titers^[3]. CCGI-1746 suppressed TNFα, IL-1β, IL-6, MCP1 and MIP-1α production in the passive anti-collagen II antibody induced arthritis (CAIA) model. Treatment with CGI-1746 at the dose of 200 mg/kg twice a week for 30 days can inhibit the growth of human OCI-MY5 xenografts in NSG mice^[4].
动物研究
剂量
Mice: 100 mg/kg^[2] (s.c.), 200 mg/kg^[3] (s.c.)

给药途径
s.c.
参考文献

动物研究
剂量	Mice: 100 mg/kg^[2] (s.c.), 200 mg/kg^[3] (s.c.)
给药途径	s.c.

[1] Kokabee L, Wang X, et al. Bruton's tyrosine kinase is a potential therapeutic target in prostate cancer. Cancer Biol Ther. 2015;16(11):1604-15.
[2] Di Paolo JA, Huang T, et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat Chem Biol. 2011 Jan;7(1):41-50.
[3] Di Paolo JA, Huang T, Balazs M, Barbosa J, Barck KH, Bravo BJ, Carano RA, Darrow J, Davies DR, DeForge LE, Diehl L, Ferrando R, Gallion SL, Giannetti AM, Gribling P, Hurez V, Hymowitz SG, Jones R, Kropf JE, Lee WP, Maciejewski PM, Mitchell SA, Rong H, Staker BL, Whitney JA, Yeh S, Young WB, Yu C, Zhang J, Reif K, Currie KS. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat Chem Biol. 2011 Jan;7(1):41-50. doi: 10.1038/nchembio.481. Epub 2010 Nov 28. PMID: 21113169.
[4] Gu C, Peng H, Lu Y, Yang H, Tian Z, Yin G, Zhang W, Lu S, Zhang Y, Yang Y. BTK suppresses myeloma cellular senescence through activating AKT/P27/Rb signaling. Oncotarget. 2017 May 23;8(34):56858-56867. doi: 10.18632/oncotarget.18096. PMID: 28915637; PMCID: PMC5593608.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7251 mL
- 8.6253 mL
- 17.2506 mL
- 5 mM
- 0.3450 mL
- 1.7251 mL
- 3.4501 mL
- 10 mM
- 0.1725 mL
- 0.8625 mL
- 1.7251 mL

技术信息

CAS号

910232-84-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C34H37N5O4

运输

蓝冰

分子量

579.69

别名

CGI-1746

溶解度

DMSO	50.0 mg/mL (86.3 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

CGI-1746 Catalog No. CSN13815

靶点选择性

请登录您的专属账户

确认信息