Category: Non-Small Cell Lung Cancer

RBN-2397 is a Selective and Orally Active NAD+ Competitive PARP7 Inhibitor

PARP is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death. The PARP family comprises 17 members. PARP1, PARP2 (inhibitor Olaparib), and PARP7 are all potential anti-cancer targets. PARP7 is a member belongs to the monoPARP family. The function...

ONO-7475 is a Selective and Orally Active AXL/Mer Inhibitor

EGFR tyrosine kinase inhibitors (EGFR-TKIs) are efficient for the treatment of non-small cell lung cancer (NSCLC) harboring EGFR mutations. However, most EGFR-positive NSCLC patients exhibit resistance to EGFR-TKIs after sometimes. The 3rd generation EGFR-TKI Osimertinib shows efficacy for overcoming EGFR T790M mutation-positive NSCLC. Anexelekto (AXL) belongs to the TAM...

TP3011 is a Potent Topoisomerase-1 Inhibitor with Anti-tumor Effect

Topoisomerases are proteins that cut the DNA backbone. Especially, topoisomerases let the cut ends twist past each other to a more relaxed configuration. Moreover, topoisomerases reseal the phosphodiester bonds in the backbone to again form an intact double helix. DNA topoisomerases I and II present in cells acts through...

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....