On November 1, 2021, Temps, Carolin; Lietha, Daniel; Webb, Emily R.; Li, Xue-Feng; Dawson, John C.; Muir, Morwenna; Macleod, Kenneth G.; Valero, Teresa; Munro, Alison F.; Contreras-Montoya, Rafael; Luque-Ortega, Juan R.; Fraser, Craig; Beetham, Henry; Schoenherr, Christina; Lopalco, Maria; Arends, Mark J.; Frame, Margaret C.; Qian, Bin-Zhi; Brunton, Valerie G.; Carragher, Neil O.; Unciti-Broceta, Asier published an article.Application of 380843-75-4 The title of the article was A conformation selective mode of inhibiting SRC improves drug efficacy and tolerability. And the article contained the following:
Despite the approval of several multikinase inhibitors that target SRC and the overwhelming evidence of the role of SRC in the progression and resistance mechanisms of many solid malignancies, inhibition of its kinase activity has thus far failed to improve patient outcomes. Here we report the small mol. eCF506 locks SRC in its native inactive conformation, thereby inhibiting both enzymic and scaffolding functions that prevent phosphorylation and complex formation with its partner FAK. This mechanism of action resulted in highly potent and selective pathway inhibition in culture and in vivo. Treatment with eCF506 resulted in increased antitumor efficacy and tolerability in syngeneic murine cancer models, demonstrating significant therapeutic advantages over existing SRC/ABL inhibitors. Therefore, this mode of inhibiting SRC could lead to improved treatment of SRC-associated disorders. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Application of 380843-75-4
The Article related to breast cancer src conformation lymphocyte ecf506 antiproliferative, Placeholder for records without volume info and other aspects.Application of 380843-75-4
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