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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-22487	SOMCL-17-016 BTK inhibitor	SOMCL-17-016 (S-016) is a potent, selective and irreversible BTK kinase inhibitor with IC50 of 0.5 nM.
PC-22306	BIIB129 BTK inhibitor	BIIB129 (BIIB-129) is a potent, selective, brain-penetrant and covalent inhibitor of BTK with binding KD of 0.63 nM, covently targets side chain nitrogen of Asn484 in BTK.
PC-22004	Civorebrutinib BTK inhibitor	Civorebrutinib (WS-413) is a novel potent, selective Bruton's tyrosine kinase (BTK) inhibitor with antineoplastic effect.
PC-20324	BGB-8035 BTK inhibitor	BGB-8035 (BGB8035) is a potent, highly selective BTK inhibitor with IC50 of 1.1 nM, potently inhibits BTK Tyr223 phosphorylation in BTK pY223 cellular assays with IC50 of 13.9 nM.
PC-49426	ACP-5862 BTK inhibitor	ACP-5862 is a major metabolite of acalabrutinib and potent and selective covalent BTK inhibitor with IC50 of 5 nM.
PC-49425	JNJ-64264681 BTK inhibitor	JNJ-64264681 is a potent, selective, covalent, irreversible BTK inhibitor with Ki of 48.5 nM, enzymatic IC50 of 558 nM.
PC-38625	CNX-774 BTK inhibitor	CNX-774 (CNX774) is a potent, selective orally active, irreversible BTK inhibitor with IC50 of <1 nM, covalently targets Cys481 of BTK.
PC-73045	XMU-MP-3 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.
PC-72757	AS-1763 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.
PC-72630	Pirtobrutinib 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.
PC-72484	KIN-8194 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.
PC-72430	TG-1701 BTK inhibitor	TG-1701 (Edralbrutinib, TG1701) is a irreversible, orally available, potent and highly specific BTK inhibitor with Kd of 3 nM, IC50 of 6.7 nM, more selective than ibrutinib.

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