Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Application of C4HCl2FN2.
Pan, Tao;Dan, Yanrong;Guo, Dafeng;Jiang, Junhao;Ran, Dongzhi;Zhang, Lin;Tian, Binghua;Yuan, Jianyong;Yu, Yu;Gan, Zongjie research published 《 Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC》, the research content is summarized as follows. Combination of anaplastic lymphoma kinase (ALK) inhibitor with histone deacetylases (HDAC) inhibitor could exert synergistically anti-proliferative effects on ALK pos. non-small cell lung cancer (NSCLC) naive or resistant cells. In this work, we designed and synthesized a series of 2,4-pyrimidinediamine derivatives as dual ALK and HDAC inhibitors based on pharmacophore merged strategy. Among which, compound I displayed the most potent and balanced inhibitory activity against ALK (IC50 = 2.1 nM) and HDAC1 (IC50 = 7.9 nM), resp. In particular, I was also potent against the frequently observed Crizotinib-resistant ALKL1196M (IC50 = 1.7 nM) as well as the Ceritinib-resistant ALKG1202R (IC50 = 0.4 nM) mutants. In antiproliferative activity assay, I exhibited impressive activity on ALK-addicted cancer cell lines at low micromole concentrations, which was comparable to that of Crizotinib and Ceritinib. Further flow cytometric anal. indicated that I could effectively induce cell death via cell apoptosis and cell cycle arrest. Taken together, these results suggested I would be a promising lead compound for the ALK-pos. NSCLC treatment, especially the Ceritinib- or Crizotinib-resistant NSCLC.
Application of C4HCl2FN2, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia