BMS-986143 is a potent, reversible inhibitor of tyrosine kinase (BTK), which has been successfully targeted by a number of irreversible tumor compounds.BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, and ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM, 19 nM, and 21 nM, respectively.
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.
 Anurag S Srivastava, et al. ACS Med Chem Lett. Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK
|Related BTK Products|
BCPyr is a new candidate BTK degradation agent (DC50 = 800 nM).
The reversible BTK kinase inhibitor BIIB091 is a highly selective phase I clinical candidate compound for multiple sclerosis.
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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