The reversible BTK kinase inhibitor BIIB091 is a highly selective phase I clinical candidate compound for multiple sclerosis.
|Solubility (25°C)||DMSO ≥ 100 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
 Anastasia Geladaris, et al. CNS Drugs. Bruton's Tyrosine Kinase Inhibitors in Multiple Sclerosis: Pioneering the Path Towards Treatment of Progression?
 Brian T Hopkins, et al. J Med Chem. Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis
 Eris Bame, et al. Clin Transl Immunology. Next-generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cells
|Related BTK Products|
BCPyr is a new candidate BTK degradation agent (DC50 = 800 nM).
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TAK-020 is a highly selective oral covalent BTK inhibitor with a promising safety and tolerability profile for both hematologic malignancies and autoimmune diseases.
|BTK inhibitor 1 (Compound 27)
BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM.
WYE-175837 is a BTK inhibitor
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