Wang, Xiaolun’s team published research in Journal of Medicinal Chemistry in 65 | CAS: 2454397-75-0

Journal of Medicinal Chemistry published new progress about 2454397-75-0. 2454397-75-0 belongs to pyrimidines, auxiliary class Aromatic Fluorinated Building Blocks, name is 7-Chloro-8-fluoropyrido[4,3-d]pyrimidine-2,4(1H,3H)-dione, and the molecular formula is C19H10Br2N2, Category: pyrimidines.

Wang, Xiaolun published the artcileIdentification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor, Category: pyrimidines, the publication is Journal of Medicinal Chemistry (2022), 65(4), 3123-3133, database is CAplus and MEDLINE.

KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of KRASG12D presents a significant challenge due to the requirement of inhibitors to bind KRASG12D with high enough affinity to obviate the need for covalent interactions with the mutant KRAS protein. Here, we report the discovery and characterization of the first noncovalent, potent, and selective KRASG12D inhibitor, MRTX1133, which was discovered through an extensive structure-based activity improvement and shown to be efficacious in a KRASG12D mutant xenograft mouse tumor model.

Journal of Medicinal Chemistry published new progress about 2454397-75-0. 2454397-75-0 belongs to pyrimidines, auxiliary class Aromatic Fluorinated Building Blocks, name is 7-Chloro-8-fluoropyrido[4,3-d]pyrimidine-2,4(1H,3H)-dione, and the molecular formula is C19H10Br2N2, Category: pyrimidines.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia