Hodges, Timothy R.’s team published research in Journal of Medicinal Chemistry in 2018 | CAS: 944401-55-2

4-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidin-2-amine(cas: 944401-55-2) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. HPLC of Formula: 944401-55-2

HPLC of Formula: 944401-55-2On October 11, 2018 ,《Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS》 was published in Journal of Medicinal Chemistry. The article was written by Hodges, Timothy R.; Abbott, Jason R.; Little, Andrew J.; Sarkar, Dhruba; Salovich, James M.; Howes, Jennifer E.; Akan, Denis T.; Sai, Jiqing; Arnold, Allison L.; Browning, Carrie; Burns, Michael C.; Sobolik, Tammy; Sun, Qi; Beesetty, Yugandhar; Coker, Jesse A.; Scharn, Dirk; Stadtmueller, Heinz; Rossanese, Olivia W.; Phan, Jason; Waterson, Alex G.; McConnell, Darryl B.; Fesik, Stephen W.. The article contains the following contents:

Son of sevenless homolog 1 (SOS1) is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS. In its active form, GTP-bound RAS is responsible for numerous critical cellular processes. Aberrant RAS activity is involved in ∼30% of all human cancers; hence, SOS1 is an attractive therapeutic target for its role in modulating RAS activation. Here, we describe a new series of benzimidazole-derived SOS1 agonists. Using structure-guided design, we discovered small mols. that increase nucleotide exchange on RAS in vitro at submicromolar concentrations, bind to SOS1 with low double-digit nanomolar affinity, rapidly enhance cellular RAS-GTP levels, and invoke biphasic signaling changes in phosphorylation of ERK 1/2. These compounds represent the most potent series of SOS1 agonists reported to date. The experimental part of the paper was very detailed, including the reaction process of 4-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidin-2-amine(cas: 944401-55-2HPLC of Formula: 944401-55-2)

4-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidin-2-amine(cas: 944401-55-2) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. HPLC of Formula: 944401-55-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia