HPLC of Formula: 3934-20-1In 2021 ,《Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Liu, Qiao; Luo, Yanli; Li, Zerui; Chen, Chen; Fang, Lei. The article conveys some information:
Utilizing osimertinib as the lead compound, this work has explored the structural modifications on the indole and pyrimidine rings of osimertinib to generate novel osimertinib derivatives I (R = acetyl, cyclopropyl, prop-2-en-1-yl, oxetan-3-yl, etc; R1 = H, CF3). The in vitro enzymic and cellular studies showed that the derivatives I possessed high selectivity towards double mutant EGFR and potent antitumor activity. Particularly, compound I (R = cyclopropyl, R1 = H), the most active compound, exhibited excellent inhibitory activity against double mutant EGFR (IC50 = 0.18 nM) and wild-type EGFR (IC50 = 2.89 nM) as well as H1975 cells (IC50 = 1.44 nM). Western blot anal. showed that I (R = cyclopropyl, R1 = H) completely inhibited double mutant EGFR and Erk phosphorylation. In vivo test using xenograft model indicated that compound I (R = cyclopropyl, R1 = H) had better antitumor efficacy than osimertinib. More importantly, I (R = cyclopropyl, R1 = H) displayed many advantages in the pharmacokinetic study, including better oral bioavailability and metabolism character.2,4-Dichloropyrimidine(cas: 3934-20-1HPLC of Formula: 3934-20-1) was used in this study.
2,4-Dichloropyrimidine(cas: 3934-20-1) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.HPLC of Formula: 3934-20-1
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia