JBJ-04-125-02 is a Mutant-Selective and Orally Active EGFR Inhibitor
Epidermal growth factor receptor (EGFR) is a transmembrane receptor protein in humans. The discovery of activating mutations in EGFR detected in 10% to 30% of patients with non–small cell lung cancer (NSCLC). In addition, it has revolutionized the treatment of this disease. Until recently, EGFR tyrosine kinase inhibitors (TKI), including...
BPI-9016M is an Orally Active and Selective Dual c-Met/AXL Inhibitor
c-Met is a membrane-spanning receptor tyrosine kinase. It has a high affinity for binding to hepatocyte growth factor (HGF). As we all know, HGF/c-Met signaling often involves activation of its downstream pathways. High-level Met gene amplification, mutation or protein overexpression can lead to aberrant activation of the HGF/c-Met pathway. In...
AGN194204 is an Orally Active and Selective RXR Agonist
Rexinoids are selective ligands for the retinoid X receptors (RXRα, RXRβ, and RXRγ). Specifically, rexinoids are multifunctional drugs that are useful for both the prevention and treatment of lung and breast cancer in preclinical animal models. Besides, retinoid X receptors heterodimerize with other receptors in the nuclear receptor superfamily. They modulate the activities of numerous steroid-like...
HKI-357 is an Irreversible Dual Inhibitor of EGFR and ERBB2
Non-small cell lung cancers with activating mutations in the kinase domain of the EGFR demonstrate dramatically, but transient, responses to the reversible tyrosine kinase inhibitors Gefitinib. To identify mechanisms of resistance to Gefitinib, Researchers used NSCLC cells harboring an activating EGFR mutation to generate multiple resistant clones. The bronchoalveolar...
PI-103 is a Potent PI3K and mTOR Inhibitor
The phosphatidylinositide 3-kinase family possesses 15 members. those members consist of four distinct classes as a basis on their structure and biological properties. As we all know, this highly conserved family of enzymes involves various aspects of cellular homeostasis and exists a decline in a number of pathophysiologic conditions....
UK 356618 is a Selective MMP-3 Inhibitor
Matrix metalloproteinase-3 (MMP-3) plays an important role in the pathology of rheumatoid arthritis (RA) and ankylosing spondylitis (AS). MMP-3 contains a signal peptide, a pro-domain, a catalytic domain, a hinge domain, and a hemopexin domain. Besides, the signal peptide is cleaved off during the secretion process and pro-domain is...
Telaglenastat is a Selective and Orally Active Inhibitor of Glutaminase 1
Tumor cells use a variety of oncogenically- and environmentally driven metabolic pathways. That aims to meet the bioenergetic and biosynthetic demands of rapid and sustained growth. One of the key nutrients is the amino acid glutamine. It is the most abundant amino acid in plasma. Small-molecule inhibitors, suppressing the...