Category: Colorectal Cancer

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)....

Lomeguatrib is a O6-Methylguanine-DNA Methyltransferase (MGMT) Inhibitor

O6-alkylguanine DNA alkyltransferase (also known as AGT, MGMT or AGAT) is a protein that in humans is encoded by the O6-methylguanine DNA methyltransferase (MGMT) gene. MGMT repairs the naturally occurring mutagenic DNA lesion O6-methylguanine back to guanine and prevents mismatch and errors during DNA replication and transcription. MGMT repairs...

Dovitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Tyrosine kinase is an enzyme that can transfer phosphate groups from ATP to tyrosine residues of specific proteins in cells. Specifically, this covalent post-translational modification is a key component of normal cell communication and homeostasis maintenance. Tyrosine kinase is an important mediator of signal cascade reaction. Besides, it plays...

Axitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Vascular endothelial growth factor (VEGF) is an important signal protein. Importantly, it is involved in angiogenesis and angiogenesis (blood vessels grow from a pre-existing vascular system). All members of VEGF family stimulate cell response by binding to tyrosine kinase receptors (VEGFRs) on the cell surface. Thus they dimerize and...

Nintedanib is an Orally Active Triple Angiokinase Inhibitor for VEGFR, FGFR and PDGFR

VEGFR are receptors for vascular endothelial growth factor (VEGF). There are three main subtypes: VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, and VEGFR3. VEGFR1 and 2 are expressed on vascular endothelial cells, whereas VEGFR3 is expressed on lymphatic endothelial. VEGFR1 and VEGFR2 play major roles in physiological as well as pathological angiogenesis. VEGFR3 can...