CGI1746 has exquisite selectivity for Btk and inhibits both auto- and transphosphorylation steps necessary for enzyme activation. CGI1746 blocks B cell receptor-dependent B cell proliferation and in prophylactic regimens reduces autoantibody levels in collagen-induced arthritis. CGI1746 decreases cytokine levels within joints and ameliorates disease. CGI1746 shows comparable efficacy to TNFα blockade and significantly reduces clinical scores, as well as joint inflammation, in mice or rats with established arthritis.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis.
Di Paolo JA, et al. Nat Chem Biol. 2011 Jan;7(1):41-50. PMID: 21113169.
|Related BTK Products|
BMS-986142 is a potent, selective, reversible BTK inhibitor, shows BTK IC50 = 0.5nM; human WB IC50 = 90 nM.
GDC-0853 is an orally BTK inhibitor with potential antineoplastic activity.
|Btk inhibitor 2
Btk inhibitor 2 (BGB-3111) is a Brutons tyrosine kinase (BTK) inhibitor.
BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective.
LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM.
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