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

Request The Product List ofBTK BTK

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-35698	BTK inhibitor 4b	BTK inhibitor 4b is a potent, highly selective inhibitors of BTK with IC50 of 4.2 and 0.9 nM against activated and unactivated BTK, respectively.
PC-62701	BTK-IN-23	BTK-IN-23 is a highly potent and selective Btk inhibitor with IC50 of 3 nM.
PC-61951	CB-988	CB-988 is a potent, highly selective, non-covalent Btk inhibitor targering ibrutinib-resistant Btk C481S mutant (IC50=0.6 nM).
PC-60404	IQS-019 mesylate	A novel, 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-42773	PCI-32765 racemate	A potent a+M7692nd highly selective Btk inhibitor with IC50 of 0.5 nM.

PREV 1 2 3 45NEXT

Select Your Country or Region

Request The Product List ofBTK BTK

Request The Product List

* Indicates a Required FieldYour information is safe with us.