910232-84-7
CGI-1746
CAS: 910232-84-7
Molecular Formula: C34H37N5O4
910232-84-7 - Names and Identifiers
910232-84-7 - Physico-chemical Properties
| Molecular Formula | C34H37N5O4 |
| Molar Mass | 579.69 |
| Density | 1.22 |
| Storage Condition | -20℃ |
| In vitro study | CGI1746 is specific for Btk and is ∼ 1,000-fold more selective than Tec and Src family kinases. In the non-ATP competitive binding assay, the dissociation constant of Btk was 1.5 nM. CGI1746 inhibits Btk activity with a new binding mode that stabilizes the inactive, non-phosphorylated enzyme conformation. CGI1746 inhibits the auto and phosphotransfer steps necessary for enzyme activation. CGI1746 completely inhibited anti-IgM-induced mouse and human B cell proliferation with IC50s at 134 nM and 42 nM, respectively, but did not affect anti-CD3 and anti-cd28-induced T cell proliferation. CGI1746 potently inhibited the proliferation of CD27 IgG B cells isolated from tonsils of four donors with an average IC50 of 112 nM. In macrophages, CGI1746 abrogated FcγRIII-induced TNFα,IL-1β, and IL-6 production. CGI1746 effectively inhibits the production of TNFα and IL-1β in human monocytes stimulated by immobilized or soluble immune complexes, and to a lesser extent inhibits IL-6 (3-fold or 8-fold higher IC50) produce. |
| In vivo study | CGI1746 abolishes B- cell dependent arthritis. Treatment with CGI174 (100 mg/kg, S.C., twice a day) resulted in a significant suppression of overall clinical arthritis (97%). In a positive anti-collagen II antibody-induced arthritis (CAIA) model, CGI1746 treatment substantially reduced mRNA and protein levels of TNFα,IL-1β ,IL-6, and MCP1 and MIP-1α. In arthritic mice and rats, CGI1746 was able to block TNFα well and significantly reduce its clinical number, while reducing joint inflammation. |
910232-84-7 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.725 ml | 8.625 ml | 17.25 ml |
| 5 mM | 0.345 ml | 1.725 ml | 3.45 ml |
| 10 mM | 0.173 ml | 0.863 ml | 1.725 ml |
| 5 mM | 0.035 ml | 0.173 ml | 0.345 ml |
Last Update：2024-01-02 23:10:35
910232-84-7 - Reference Information
| biological activity | CGI1746 is a potent, highly selective, small molecule inhibitor of Btk with an IC50 of 1.9 nM. |
Last Update：2024-04-09 20:48:19
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Product Name: CGI-1746 Visit Supplier Webpage Request for quotationCAS: 910232-84-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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