Tolebrutinib, also known as SAR442168, is a Bruton tyrosine kinase (BTK) inhibitor, with IC50 values of 0.4 nM and 0.7 nM in Ramos B cells and HMC microglia cells, respectively. Tolebrutinib blocks the BCR-mediated activation (IC50=10 nM) and Fc receptor activation (IC50=166 and 9.6 nM for FcεR and FcγR, repectively) of immune cells. Tolebrutinib inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM.
|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.
|Solubility||DMSO 80 mg/mL|
|Related BTK Products|
Remibrutinib (LOU064) is a potent and highly selective covalent Inhibitor of Bruton's Tyrosine Kinase (BTK) with IC50 value of 1 nM.
Orelabrutinib is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).
Zanubrutinib (BGB-3111) is a potent and highly selective small molecule inhibitor of Bruton's tyrosine kinase (BTK).
ARQ 531 is a potent reversible inhibitor of BTK (IC50 = 0.85 nM), exhibits potent antitumor activity in ibrutinib-resistant diffuse large B-cell lymphoma.
PCI-29732 is a potent, reversible BTK inhibitor.
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