Henry, James R. published the artcileDiscovery of 1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a Pan-RAF Inhibitor with Minimal Paradoxical Activation and Activity against BRAF or RAS Mutant Tumor Cells, Name: 1-Bromo-4-fluoro-2-methylbenzene, the main research area is antitumor RAF inhibitor LY3009120 preparation structure activity cancer.
The RAS-RAF-MEK-MAPK cascade is an essential signaling pathway, with activation typically mediated through cell surface receptors. The kinase inhibitors vemurafenib and dabrafenib, which target oncogenic BRAF V600E, have shown significant clin. efficacy in melanoma patients harboring this mutation. Because of paradoxical pathway activation, both agents were demonstrated to promote growth and metastasis of tumor cells with RAS mutations in preclin. models and are contraindicated for treatment of cancer patients with BRAF WT background, including patients with KRAS or NRAS mutations. To eliminate the issues associated with paradoxical MAPK pathway activation and to provide therapeutic benefit to patients with RAS mutant cancers, we sought to identify a compound not only active against BRAF V600E but also wild type BRAF and CRAF. On the basis of its superior in vitro and in vivo profile, compound 13 was selected for further development and is currently being evaluated in phase I clin. studies.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 452-63-1 belongs to class bromides-buliding-blocks, name is 1-Bromo-4-fluoro-2-methylbenzene, and the molecular formula is C7H6BrF, Name: 1-Bromo-4-fluoro-2-methylbenzene.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary