JS25, a Selective and Covalent BTK Inhibitor, Acts by Segregating Tyr551
BTK, Bruton’s tyrosine kinase, belongs to the cytoplasmatic kinases TEC subfamily. BTK involves in immune regulation, and is activated by Src kinases. Then BTK leads to phospholipase-Cγ (PLCγ) phosphorylation, Ca2+ mobilization, and NF-κB/MAP activation. Meanwhile, BTK increases proinflammatory cytokines IL-6 and IL-10 production and controls integrin-mediated B-cells adhesion. Moreover,...
JBJ-09-063 is a Mutant-Selective Allosteric EGFR Inhibitor
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor. And the IC50 values are 0.147 nM, 0.063 nM, 0.083 nM, and 0.396 nM for EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797S, and EGFRLT/L747S, respectively. JBJ-09-063 is remarkably effective at inhibiting cell growth. And it also leads to a significant increase in apoptosis. JBJ-09-063 is effective...
EAI001 is a Selective Mutant EGFR Allosteric Inhibitor
Epidermal growth factor receptor (EGFR) belongs to the ErbB family of receptor tyrosine kinases (RTKs). Specifically, EGFR belongs to a receptor family, which contains three additional proteins, namely ErbB-2, ErbB-3, and ErbB-4. These proteins and EGF family growth factors form a comprehensive system. Besides, EGFR participates in cell growth...
BI-1622 is an Orally active and Selective HER2 Inhibitor
BI-1622 is an orally active, potent, and highly selective HER2 (ERBB2) inhibitor, with IC50 values of 7.8, 7.1, <5.3 nM for HER2WT, HER2YVMA, EGFRWT, respectively. Besides, BI-1622 shows greater than 25-fold selectivity over EGFR. Moreover, BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models. HER2 is a member...
Lapatinib is a Potent Inhibitor of the ErbB-2 and EGFR Tyrosine Kinase Domains
Growth factors and their transmembrane receptor tyrosine kinase play important roles in cell proliferation, survival, migration, and differentiation. Additionally, Epidermal growth factor (EGF)-like proteins stimulates cells to divide by activating members of the EGF receptor (EGFR) family. Many types of human tumor cells growth and development are related to the...
Avitinib is an Irreversible, Mutant-Selective EGFR Inhibitor
The epidermal growth factor receptor (EGFR) belongs to the ErbB family (also known as the EGFR family) of receptor tyrosine kinases (RTK). EGFR family comprises four distinct receptors: the EGFR (ErbB1, HER1), ErbB-2 (HER2, neu in rodents), ErbB-3 (HER3) and ErbB-4 (HER4). It is worth mentioning that EGFR family...
Almonertinib is an Orally Active and Irreversible EGFR Inhibitor
Lung cancer is one of the most common malignant tumors in the world. Its lethality ranks the first among many malignant tumors. In addition, the overexpression of the human ATP-binding cassette (ABC) drug transporter ABCB1 (P-gp) or ABCG2 (BCRP) in cancer cells often contributes significantly to the development of...