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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-42396	(±)-Zanubrutinib	The active enantiomer of Zanubrutinib, a potent, selective and orally available Btk inhibitor.
PC-45739	Fenebrutinib BTK inhibitor	Fenebrutinib (RG-7845, GDC-0853) is an orally bioavailable, selective, non-covalent and reversible BTK inhibitor with IC50 of 2-9 nM.
PC-45400	PCI-29732 BTK inhibitor	APCI-29732 is a potent, selective and irreversible Btk inhibitor with biochemical Ki of 8.2 nM.
PC-44705	ONO-4059 hydrochloride mutant EGFR inhibitor	ONO-4059 (Tirabrutinib) hydrochloride is potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.
PC-44704	Tirabrutinib mutant EGFR inhibitor	Tirabrutinib (ONO 4059, GS 4059) is a potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.
PC-46006	QL-47 BTK inhibitor	QL-47 is a potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM.
PC-42336	Evobrutinib BTK inhibitor	Evobrutinib (M2951, MSC2364447C, MSC 2364447) is a potent, highly selective, covalent and oral BTK inhibitor with enzyme IC50 of 8.9 nM.
PC-45403	RN-486 BTK inhibitor	RN-486 is a potent and selective BTK inhibitor with IC50 of 4 nM in enzymatic assays.
PC-42772	Ibrutinib	Ibrutinib (PCI-32765,PCI32765) is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM.
PC-45383	Acalabrutinib BTK inhibitor	Acalabrutinib (ACP-196) is a potent, irreversible, covalent second-generation BTK inhibitor with IC50 of 3 nM.
PC-45399	LFM-A13 BTK inhibitor	LFM-A13 is a highly specific inhibitor of BTK with Ki of 1.4 uM, IC50 of 17.2 uM, shows no activity against EGFR, IRK, JAK1, JAK3, or HCK.
PC-45402	AVL-292 besylate BTK inhibitor	AVL-292 besylate (Spebrutinib, CC-292) is a highly selective, covalent Btk inhibitor with IC50 of <1 nM.

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