LFM-A13 - CAS 244240-24-2
Catalog number: 244240-24-2
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Polo-like Kinase (PLK)
LFM-A13 is a specific Bruton's tyrosine kinase (BTK) with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK.
LFM A13; LFM-A13; LFM A13
Canonical SMILES:
1.Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders.
Robak T1, Robak E. Expert Opin Investig Drugs. 2012 Jul;21(7):921-47. doi: 10.1517/13543784.2012.685650. Epub 2012 May 22.
INTRODUCTION: In the last few years, several tyrosine kinase inhibitors (TKIs) have been synthesized and become available for preclinical studies and clinical trials. This article summarizes recent achievements in the mechanism of action, pharmacological properties, and clinical activity and toxicity, as well as the emerging role of TKIs in lymphoid malignancies, allergic diseases, and autoimmune disorders.
2.[Role of non-receptor tyrosine kinase Tec in the production of pro-inflammatory cytokines from macrophages induced by endotoxin/lipopolysaccharide].
Wang C1, Wang F1, Zhou B1, Qiu L1, Wang J1, Liu S1, Chen X2. Zhonghua Shao Shang Za Zhi. 2015 Feb;31(1):11-5.
OBJECTIVE: To investigate the role of non-receptor tyrosine kinase Tec in the production of TNF-α and IL-1β from macrophages induced by LPS and its related mechanism.
3.Ibrutinib and novel BTK inhibitors in clinical development.
Akinleye A1, Chen Y, Mukhi N, Song Y, Liu D. J Hematol Oncol. 2013 Aug 19;6:59. doi: 10.1186/1756-8722-6-59.
Small molecule inhibitors targeting dysregulated pathways (RAS/RAF/MEK, PI3K/AKT/mTOR, JAK/STAT) have significantly improved clinical outcomes in cancer patients. Recently Bruton's tyrosine kinase (BTK), a crucial terminal kinase enzyme in the B-cell antigen receptor (BCR) signaling pathway, has emerged as an attractive target for therapeutic intervention in human malignancies and autoimmune disorders. Ibrutinib, a novel first-in-human BTK-inhibitor, has demonstrated clinical effectiveness and tolerability in early clinical trials and has progressed into phase III trials. However, additional research is necessary to identify the optimal dosing schedule, as well as patients most likely to benefit from BTK inhibition. This review summarizes preclinical and clinical development of ibrutinib and other novel BTK inhibitors (GDC-0834, CGI-560, CGI-1746, HM-71224, CC-292, and ONO-4059, CNX-774, LFM-A13) in the treatment of B-cell malignancies and autoimmune disorders.
4.Bruton tyrosine kinase inhibitors: a promising novel targeted treatment for B cell lymphomas.
Aalipour A1, Advani RH. Br J Haematol. 2013 Nov;163(4):436-43. doi: 10.1111/bjh.12573. Epub 2013 Sep 24.
Constitutive or aberrant signalling of the B cell receptor signalling cascade has been implicated in the propagation and maintenance of a variety of B cell malignancies. Small molecule inhibitors of Bruton tyrosine kinase (BTK), a protein early in this cascade and specifically expressed in B cells, have emerged as a new class of targeted agents. There are several BTK inhibitors, including ONO-WG-307, LFM-A13, dasatinib, CC-292, and PCI-32765 (ibrutinib), in preclinical and/or clinical development of which ibrutinib is currently in phase III trials. Recent clinical data suggest significant activity of ibrutinib as a first in class oral inhibitor of BTK. This review provides an overview of ongoing clinical studies of BTK inhibitors.
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CAS 244240-24-2 LFM-A13

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