Safety of 1-Phenylurea. Recently I am researching about AURORA KINASE; MEK INHIBITION; DRUG DESIGN; MECHANISMS; RESISTANCE; BRAF; KIT; IDENTIFICATION; VEMURAFENIB; SIMULATION, Saw an article supported by the University of Pisa [PRA_2017_51]. Published in NATURE PUBLISHING GROUP in LONDON ,Authors: Quattrini, L; Coviello, V; Sartini, S; Di Desidero, T; Orlandi, P; Ke, YY; Liu, KL; Hsieh, HP; Bocci, G; La Motta, C. The CAS is 64-10-8. Through research, I have a further understanding and discovery of 1-Phenylurea
Melanoma is the most serious form of skin cancer but its medication is still far from being safe and thoroughly effective. The search of novel therapeutic approaches represents therefore a health emergency to push through eagerly. In this study, we describe a novel class of dual c-Kit/Aur inhibitors, characterized by a 1,2,4-triazole core and developed by a structure-based optimization of a previously developed hit, and report the evidence of their significance as drug candidates for the treatment of melanoma. Compound 6a, merging the best inhibitory profile against the target kinases, showed anti-proliferative efficacy against the human melanoma cell lines A2058, expressing the BRAFV600D mutation, and WM266-4, expressing BRAF V600E. Significantly, it displayed also a highly synergistic profile when tested in combination with vemurafenib, thus proving its efficacy not only per se but even in a combination therapy, which is nowadays acknowledged as the cornerstone approach of the forthcoming tumour management.
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Reference:
Thiomorpholine – Wikipedia,
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