產(chǎn)品描述: | CGI-1746 is a potent and highly selective inhibitor of the Btk with IC50 of 1.9 nM. |
靶點(diǎn): |
IC50: 1.9 nM (Btk);BTK;?Autophagy |
體內(nèi)研究: |
CGI1746 abrogates B cell-dependent arthritis. CGI1746 treatment (100 mg/kg, s.c, twice-daily dosing) results in significant inhibition (97%) of overall clinical arthritis scores. CGI1746 treatment substantially reduces TNFα, IL-1β and IL-6, as well as MCP1 and MIP-1α on both the mRNA and protein level in the passive anti-collagen II antibody-induced arthritis (CAIA) model. CGI1746 shows comparable efficacy to TNFα blockade and significantly reduces clinical scores, as well as joint inflammation, in mice or rats with established arthritis |
參考文獻(xiàn): |
1. Di Paolo, Julie A. et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nature Chemical Biology (2011), 7(1), 41-50 2. Kokabee L, et al. Bruton's tyrosine kinase is a potential therapeutic target in prostate cancer. Cancer Biol Ther. 2015;16(11):1604-15 |
溶解性: |
DMSO : ≥ 50 mg/mL (86.25 mM) |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
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 |
50 mM |
0.035 ml |
0.173 ml |
0.345 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |