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...
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....
AMG-510 is a First-in-Class, Orally Active, and Selective KRAS G12C Inhibitor
The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. They are involved in tumor cell growth and survival. Somatic, activating mutations in KRAS are a hallmark of cancer. Furthermore, they prevent the association of GTPase-activating proteins, thus stabilizing effector binding and enhancing KRAS signaling....
BI-4020 is an Orally Active EGFR Tyrosine Kinase Inhibitor
The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase that transduces mitogenic signals. When EGFR carries an activating mutation, it can be an oncogenic driver in lung tumors. Notably, Since additional mutation in the EGFR kinase domain that confers resistance to TKIs, lung cancer patients relapse within...
GNE-618 is a Orally Active NAMPT Inhibitor
Nicotinamide adenine dinucleotide (NAD) is a critical metabolite for a range of cellular reactions. NAD is an essential coenzyme involved in cellular redox reactions and is a substrate for NAD-dependent enzymes. Especially, Nicotinamide phosphoribosyltransferase (Nampt) is an enzyme necessary for NAD synthesis. Nampt catalyzes the rate-limiting step leading to...
CG-200745, a HDAC Inhibitor, Induces the Accumulation of p53
Histone deacetylase (HDAC) inhibits are considered to be promising agents that can be used as treatments for cancer. CG-200745 is a novel and potent hydroxamate-based pan-HDAC inhibitor. CG-200745 has the hydroxamic acid moiety to bind zinc at the bottom of the catalytic pocket. We will introduce its anti-tumorigenic property...