Tag: colorectal cancer

Sotorasib (AMG-510) is an Orally Bioavailable KRAS G12C Covalent Inhibitor

The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. KRAS oncoprotein regulates tumor cell growth and survival. However, KRAS also is the most frequently mutated oncogene in cancer and encodes a key signaling protein in tumors. In addition, KRASG12C mutant is present in approximately...

Opnurasib (JDQ-443) is an Orally Active KRAS G12C Inhibitor

Kirsten rat sarcoma (KRAS) is a member of the RAS family. KRAS is a key regulator of signaling pathways responsible for cell proliferation, differentiation, and survival. KRAS mutations are genetic drivers of multiple cancer types, especially colorectal cancer (CRC), pancreatic ductal adenocarcinoma (PDAC), and non-small cell lung cancer (NSCLC)....

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,...