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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 CAS No. Information
PC-38125

Remibrutinib

1787294-07-8 Remibrutinib (LOU064) is a potent, highly selective covalent BTK inhibitor with IC50 of 1.3 nM.
PC-38012

PRN473

1581714-49-9 PRN473 (Atuzabrutinib, SAR 444727, PRN-473) is a potent, selective, covalent reversible BTK inhibitor.
PC-35328

ARQ-531

2095393-15-8 ARQ-531 (ARQ531) is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM, respectively.
PC-63295

BMS-986195

1912445-55-6 BMS-986195 (Branebrutinib) is a novel potent, selective, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK) with IC50 of 0.1 nM.
PC-62583

PRN 1008

1575596-29-0 PRN1008 is a novel reversible, covalent and oral inhibitor of BTK with biochemical IC50 of 1.3 nM..
PC-60536

Poseltinib

1353552-97-2 Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.
PC-60535

(S)-Zanubrutinib

1691249-45-2 (S)-Zanubrutinib (BGB3111) is a potent, selective and orally available Btk inhibitor.

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