Category: Colorectal Cancer

Enavatuzumab (PDL192) is a Humanized IgG1 Monoclonal Antibody Targeting TWEAK

Antibody-dependent cytotoxicity (ADCC) is a cell-mediated immune defense mechanism. The effector cells of the immune system actively cleave target cells, and their membrane surface antigens are bound by specific antibodies. Besides, it is one of the mechanisms by which antibodies, as part of the humoral immune response, can limit...

Nanrilkefusp alfa is a Selective and Potent Agonist Fusion Protein of IL-15.

IL-15 is a cytokine involved in the regulation of the innate immune system. It stimulates the proliferation and activation of natural killer (NK) cells and memory CD8+ T cells. And also it promotes the secretion of a variety of cytokines. Moreover, IL-15 enhances the antibody-dependent cytotoxicity (ADCC) of antibodies. Specifically,...

Tigatuzumab (CS-1008) is a Humanized Death Receptor 5 (DR5) IgG1 mAb

Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), a member of the TNF superfamily of cytokines, is a type 2 membrane protein expressed in the majority of normal tissues. TRAIL can undergo protease cleavage, resulting in a soluble form able to bind to TRAIL death receptors (DRs). Moreover, TRAIL induces apoptosis...

LY3177833 is an Orally Active CDC7 and pMCM2 Inhibitor

CDC7 is a serine/threonine kinase and plays an important role in the initiation of DNA replication. . In this article, we will introduce a potent CDC7 and pMCM2 inhibitor LY3177833. LY3177833 has an  IC50 of 3.3 nM against CDC7. Upregulation of CDC7 has been observed in numerous tumor cell...

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...

LDN-211904 is a Potent and Selective EphB3 Inhibitor for Colorectal Cancer Research

LDN-211904  is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. Besides, LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. What’s more, LDN-211904 oxalate with cetuximab could effectively inhibit STAT3-activated CSC stemness and cetuximab resistance in colorectal cancer. LDN-211904 oxalate is a potent EphB3 inhibitor. Besides,...

Pimasertib is a Highly Selective and ATP non-Competitive Allosteric Inhibitor of MEK1/2

The RAS/RAF/MEK/MAPK and the PTEN/PI3K/AKT/mTOR pathways are key regulators of proliferation and survival in human cancer cells. RAF is a serine/threonine kinase that activates downstream signals in response to activated GTP-bound RAS by phosphorylating MEK  (MEK1 and MEK2). They in turn phosphorylate and activate MAPK (or ERK1 and ERK2)....