Poseltinib (HM71224; LY3337641; HM-71224; LY-3337641) is a covalent/irreversible BTK (Bruton’s tyrosine kinase) tyrosine kinase inhibitor with the potential for the treatment of rheumatoid arthritis. Poseltinib acts by irreversibly binding to the cysteine 481 residue in the active site of BTK and thus inhibiting Btk with an IC50 of 1.95 nM.

Spebrutinib (formerly AVL-292; CC-292; SBT) is a covalent/irreversible, orally bioactive, and highly selective inhibitor of Bruton’s agammaglobulinemia tyrosine kinase/BTK inhibitor with potential antitumor activity. It inhibits BTK with an IC50 of<0.5 nM, and exhibits > 1400-fold higher selectivity for BTK over the other kinases.

Rilzabrutinib (PRN-1008) is a novel, highly potent, and reversible covalent inhibitor of BTK (Bruton’s Tyrosine Kinase) being studied for treating rheumatoid arthritis. It inhibits BTK with an IC50 of 1.3 nM. BTK is a Tec family tyrosine kinase, is critical in immune pathways as an essential intracellular signaling element, participating in both adaptive and immune […]

LFM-A13 (LFM-A1-3) is a novel, potent and specific Bruton’s tyrosine kinase (BTK) inhibitor with potential anticancer activity. It inhibits BTK with an IC50 of 2.5 μM, and shows >100-fold selectivity over other protein kinases such as JAK1, JAK2, HCK, EGFR,and IRK. LFM-A13 inhibited recombinant BTK expressed in a baculovirus expression vector system. Besides its remarkable […]

BTK inhibitor 27, compound 27 in the cited reference below, is a pyrrolo[2,3-d]pyrimidine based BTK inhibitor with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM. Btk is a tyrosine kinase dysregulated in several B-cell malignancies and autoimmune diseases, and this has given rise […]

Nemtabrutinib (ARQ531; ARQ-531; MK-1026) is a novel, potent, orally bioavailable, and reversible / non-covalent BTK (Bruton’s Tyrosine Kinase) inhibitor with potential antitumor activity. It inhibits WT-BTK and C481S-BTK with IC50s of 0.85 nM and 0.39 nM, respectively.

Pirtobrutinib HCl (formerly known as LOXO-305; RXC 005), the hydrochloride salt of Pirtobrutinib, is a novel, potent, selective non-covalent / reversible Bruton’s tyrosine kinase (BTK) inhibitor that is under investigation for the treatment of cancer. It is currently being studied in a global Phase 1/2 clinical trial. BTK plays a key role in the B-cell […]