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Bruton's tyrosine kinase (Btk or BTK) is a kinase that plays a crucial role in B-cell development. BTK plays a crucial role in B cell maturation as well as mast cell activation through the high-affinity IgE receptor. BTK has emerged as a promising drug target for multiple diseases, particularly haematopoietic malignancies and autoimmune diseases related to B lymphocytes. Considerable progress has been made in the development of irreversible inhibitors, most of which target the SH3 pocket and the cysteine 481 residue of BTK.

Ibrutinib, a first-in-class BTK inhibitor, has demonstrated high response rates in both relapsed/refractory and treatment naïve chronic lymphocytic leukemia (CLL). However, scientists identified a structurally novel mutation (BTKT316A) in the SH2 domain, but not kinase domain, of Bruton tyrosine kinase which was associated with disease relapse.

Acalabrutinib (ACP-196) demonstrated higher biochemical and cellular selectivity than ibrutinib and spebrutinib. Acalabrutinib is a BTK inhibitor with key pharmacologic differentiators versus ibrutinib and spebrutinib and is currently being evaluated in clinical trials. More BTK inhibitors (GDC-0834, CGI-560, CGI-1746, HM-71224, CC-292, and ONO-4059, CNX-774, LFM-A13) are under inverstigation in the treatment of B-cell malignancies and autoimmune disorders.



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5. Barf T, et al. J Pharmacol Exp Ther. 2017 Nov;363(2):240-252.

Cat. No. Product Name Information


BTK inhibitor

Civorebrutinib (WS-413) is a novel potent, selective Bruton's tyrosine kinase (BTK) inhibitor with antineoplastic effect.


BTK inhibitor

XMU-MP-3 is a potent, selective, noncovalent BTK inhibitor with IC50 of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation.


BTK inhibitor

Milrebrutinib (AS1763, AS-1763) is a potent, selective, noncovalent, and orally available inhibitor of BTK with IC50 of 0.85 nM and 0.99 nM for wild-type BTK and C481S mutant, respectively.


BTK inhibitor

Pirtobrutinib (LOXO-305, LY3527727, RXC-005) is a highly potent and selective non-covalent BTK inhibitor with IC50 of 5.69 nM, shows nanomolar potency against both wild-type and C481-mutated BTK.


HCK BTK inhibitor

KIN-8194 (KIN8194) is a highly potent dual HCK and BTK inhibitor with IC50 of <0.495 and 0.915 nM, respectively.


BTK inhibitor

BIIB091 (BIIB 091) is a novel potent, selective, reversible BTK inhibitor with IC50 of 0.45 nM in enzymatic assays.


BTK inhibitor

Tolebrutinib (PRN2246, SAR442168, BTK168) is a potent, selective oral brain-penetrant BTK inhibitor with IC50 of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.


BTK inhibitor

Remibrutinib (LOU064) is a potent, highly selective covalent BTK inhibitor with IC50 of 1.3 nM.


BTK inhibitor

PRN473 (Atuzabrutinib, SAR 444727, PRN-473) is a potent, selective, covalent reversible BTK inhibitor.


BTK inhibitor

Nemtabrutinib (ARQ531) is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM, respectively.


BTK inhibitor

ABBV-105 (ABBV105) is a potent, selective, irreversible, covalent inhibitor of BTK with IC50 of 0.18 uM.


BTK inhibitor

BMS-986195 (Branebrutinib) is a novel potent, selective, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK) with IC50 of 0.1 nM.

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