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CGI-1746

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Chemical Structure| 910232-84-7 同义名 : -
CAS号 : 910232-84-7
货号 : A147108
分子式 : C34H37N5O4
纯度 : 98%
分子量 : 579.689
MDL号 : MFCD18782602
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(86.25 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BTK

    BTK, IC50:1.9 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.63mL

1.73mL

0.86mL

17.25mL

3.45mL

1.73mL
参考文献

[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.