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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.

References:

1. Winer ES, et al. Expert Opin Investig Drugs. 2012 Mar;21(3):355-61.

2. Kharfan-Dabaja MA, et al. Leukemia. 2014 Mar;28(3):507-17.

3. Aw A, et al. Drugs Aging. 2017 Jul;34(7):509-527.

4. Sharma S, et al. Oncotarget. 2016 Oct 18;7(42):68833-68841.

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

Cat. No.	Product Name	Information
PC-72316	ONO-WG-307 BTK inhibitor	ONO-WG-307 is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM.
PC-72229	BIIB091 BTK inhibitor	BIIB091 (BIIB 091) is a novel potent, selective, reversible BTK inhibitor with IC50 of 0.45 nM in enzymatic assays.
PC-72114	Luxeptinib Trk inhibitor	Luxeptinib (CG-806) is an orally bioavailable multikinase inhibitor with nanomolar potency against BTK, FLT3, TRK, STE/MAPK and Aurora kinase clusters.
PC-38193	Tolebrutinib 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.
PC-38125	Remibrutinib BTK inhibitor	Remibrutinib (LOU064) is a potent, highly selective covalent BTK inhibitor with IC50 of 1.3 nM.
PC-38012	PRN473 BTK inhibitor	PRN473 (Atuzabrutinib, SAR 444727, PRN-473) is a potent, selective, covalent reversible BTK inhibitor.
PC-35698	Sofnobrutinib BTK inhibitor	Sofnobrutinib (AS-0871, BTK inhibitor 4b) is a potent, highly selective, non-covalent inhibitor of BTK with IC50 of 4.2 and 0.9 nM against activated and unactivated BTK, respectively.
PC-35328	ARQ-531 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.
PC-35203	ABBV-105 BTK inhibitor	ABBV-105 (ABBV105) is a potent, selective, irreversible, covalent inhibitor of BTK with IC50 of 0.18 uM.
PC-63295	BMS-986195 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.
PC-42817	CGI-1746 BTK inhibitor	CGI-1746 is a potent, highly selective, second-generation BTK inhibitor with IC50 of 1.9 nM, displays 1,000-fold selectivity over Tec and Src family kinases.
PC-62888	GNE-431 BTK inhibitor	GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively.

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