Category: 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...

AMG 511 is an Orally Active pan-PI3K Inhibitor

The PI3K signaling network has a central role in several cellular processes critical to the initiation and progression of cancer, including growth, survival, and metabolism. The PI3K family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger that plays a critical role in important cellular functions such as...

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...

NU1025 is a Potent PARP Inhibitor with Anti-Cancer and Neuroprotective Activity

Excessive glutamate release, Ca++ overload, free radical generation, poly (ADP-ribose) polymerase (PARP) overactivation are the main events of neuronal cell death in ischemic stroke. Besides, stroke is a third leading cause of death after heart diseases and cancer and a major cause of disabilities throughout the world. Moreover, excessive...

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...