| Name | CGI-1746 |
| Description | CGI1746 is a potent and highly selective small-molecule Btk inhibitor with IC50 of 1.9 nM. |
| Cell Research | CGI-1746 is dissolved in DMSO. 5×103?DU145 cells or 104?LNCaP cells per well, grown on 96 well plates for 24h, are treated with 1 to 30?μM BTK inhibitors. Cells are fixed after 72h with 2.5% formaldehyde, and stained with Hoechst 33342. Control cells are treated with DMSO. Cell images are acquired using an IN Cell Analyzer 2200 high content imaging system, with a 20X objective. At least 9 fields are imaged per single well of each experiment. Cell numbers are determined and statistics performed using IN Cell Investigator 3.4 high content image analysis software. Each experiment is replicated 3 times, and data are presented as mean±SD. Results are considered significant if p < 0.05. |
| In vitro | Treatment with CGI1746 at a dose of 100 mg/kg, administered subcutaneously twice daily, resulted in a significant suppression (97%) of overall clinical arthritis symptoms. In a positive anti-collagen type II antibody-induced arthritis model, CGI1746 significantly reduced levels of TNFα, IL-1β, and IL-6, as well as MCP-1 and MIP-1α mRNA and protein. In mice and rats with arthritis, CGI1746 demonstrated superior efficacy compared to TNFα blockade, significantly lowering clinical scores while also reducing joint inflammation. |
| In vivo | CGI1746 effectively inhibits the proliferation of CD27+IgG+ B cells isolated from the tonsils of four donors, with an average IC50 of 112 nM. It completely suppresses B cell proliferation induced by anti-IgM in both mice and humans, with IC50s of 134 nM and 42 nM, respectively, yet does not affect T cell proliferation induced by anti-CD3 and anti-CD28. In macrophages, CGI1746 eliminates the production of TNFα, IL-1β, and IL-6 triggered by FcγRIII. It also efficiently inhibits the production of TNFα and IL-1β in human monocytes stimulated by immobilized or soluble immune complexes, and to a lesser extent, reduces IL-6 production. CGI1746 shows high specificity and selectivity for Btk, being ~1,000 times more selective than for Tec and Src family kinases. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 95 mg/mL (163.9 mM)
Ethanol : 33 mg/mL (57 mM)
|
| Keywords | Inhibitor | Bruton tyrosine kinase | Autophagy | CGI-1746 | CGI1746 | CGI 1746 | inhibit | Btk |
| Inhibitors Related | Stavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Immuno-Oncology Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
