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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-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.
PC-62583	PRN1008 BTK inhibitor	Rilzabrutinib (PRN1008) is a potent, selective, covalent reversible BTK inhibitorwith IC50 of 1.3 nM.
PC-61491	BMS-935177 BTK inhibitor	BMS-935177 is a potent and selective, orally bioavailable, reversible BTK inhibitor with IC50 of 2.8 nM.
PC-60536	Poseltinib BTK inhibitor	Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.
PC-60535	Zanubrutinib BTK inhibitor	Zanubrutinib (BGB3111) is a potent, selective and orally available Btk inhibitor with IC50 of 0.3 nM.
PC-50001	Vecabrutinib	Vecabrutinib (SNS-062) is a potent, reversible, non-covalent BTK inhibitor with IC50 of 2.9 and 4.4 nM for WT BTK and C481S BTK, respectively.
PC-60422	BMS-986142	BMS-986142 (BMS 986142) is a potent, selective and reversible BTK inhibitor with IC50 of 0.5 nM.
PC-60403	IQS-019 BCR signaling inhibitor	IQS-019 is a potent inhibitor of most upstream tyrosine kinases in BCR signaling pathway, inhibits BCR kinases Lyn, Syk and Btk with IC50 of 0.15 uM, 1.6 uM and 2.1 uM, respectively.
PC-60364	G-744	G-744 is a highly potent, selective inhibitor of BTK with biochemical Ki of 1.28 nM.
PC-70205	KS-99	KS-99 (KS99) is a novel dual inhibitor of BTK and tubulin polymerization.
PC-60272	MDVN-1003 BTK/PI3Kδ inhibitor	MDVN-1003 (MDVN1003) is a first-in-class, selective, orally bioavailable, dual inhibitor of BTK and PI3Kδ kinases with IC50 of 32.3 nM and 16.9 nM, respectively.

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