Category: Lung Cancer

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...

BI-0474 is a Potent KRAS G12C inhibitor

K-Ras protein is a kind of GTPase. Specifically, it is a kind of enzyme that converts nucleotide guanosine triphosphate (GTP) to guanosine diphosphate (GDP). In this way, the K-Ras protein acts like a switch. Besides, KRAS is the most frequently changed homotype in NSCLC cases with RAS mutation. Moreover,...

Serplulimab (HLX 10) is humanized monoclonal anti-PD-1 antibody

PD-1 (Programmed cell death protein 1; CD279) is an immune checkpoint. PD-1 is a cell surface receptor that belongs to the immunoglobulin superfamily. Besides, It shows a role in regulating the immune system’s response by down-regulating the immune system. Meanwhile, this compound promotes self-tolerance by suppressing T-cell inflammatory activity....

BT5528 is a Bicyclic Peptide Toxin Conjugate, an EphA2 Activator.

The tyrosine kinase EphA2 belongs to the Eph receptor family and is produced in large quantities in tumor tissues. Specifically, its content is relatively low in most normal adult tissues. The liver ligand receptor (Eph) is the most important receptor tyrosine kinase (RTK). Besides, Eph receptor signal transduction contributes...

G12Si-5 is a K-Ras G12S Mutant Covalent Inhibitor

KRAS (Kirsten rat sarcoma virus) is one of the most commonly altered oncogenes in human cancers. Recurrent oncogenic mutations in KRAS can reprogram glutamine metabolism to increase the production of NADPH to control ROS. Besides, mutant KRAS promotes the expression of nucleotide synthesis genes and controls glucose uptake and...

LCS3 is a Glutathione Disulfide Reductase (GSR) and TXNRD1 Inhibitor

Glutathione Disulfide Reductase (GSR), also known as glutathione reductase (GR), catalyzes the reduction of glutathione disulfide (GSSG) to glutathione (GSH) in the presence of NADPH and flavin adenine dinucleotide (FAD). GSH acts as a scavenger of reactive oxygen species (ROS) such as free radicals, peroxides, lipid peroxides and heavy...

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...