BTK (inhibitors, antagonists, agonists)-ProbeChem.com

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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-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.
PC-45401	AVL-292 BTK inhibitor	AVL-292 (Spebrutinib, CC-292) is a highly selective, covalent Btk inhibitor with IC50 of <1 nM.
PC-45570	ONO-4059 analog BTK inhibitor	ONO-4059 analog is a highly potent and selective Btk inhibitor with IC50 in the sub-nM range, analog of ONO-4059.
PC-42104	Ibrutinib-biotin	Ibrutinib-biotin is a chemical probe that consists of Ibrutinib linked to biotin via a long chain linker, has IC50 of 0.755-1.02 nM for Btk kinase.
PC-23189	Orelabrutinib BTK inhibitor	Orelabrutinib (ICP-022) is a potent, selective, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 1.6 nM.
PC-23081	Rocbrutinib BTK inhibitor	Rocbrutinib (LP-168) is a highly selective next-generation inhibitor of BTK that can bind wild-type BTK covalently and C481-mutated BTK non-covalently (reversibly), shows preclinical activity in resistant CLL models.
PC-22200	PF-06658607 BTK inhibitor	PF-06658607 is a potent, selective and irreversible Brutons tyrosine kinase (BTK) inhibitor.
PC-22003	Cinsebrutinib BTK inhibitor	Cinsebrutinib is a novel potent, selective Bruton's tyrosine kinase (BTK) inhibitor.
PC-21570	DZD8586 LYN/BTK dual inhibitor	DZD8586 is an oral, non-covalent, BBB penetrant LYN and BTK dual inhibitor, overcomes resistance mutations to the approved covalent and non-covalent BTK inhibitors.
PC-21379	TL-895 BTK inhibitor	TL-895 (M7583) is a potent, highly selective, ATP-competitive, second-generation, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with biochemical IC50 of 1.5 nM.

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