Recently I am researching about CELL LUNG-CANCER; IRREVERSIBLE INHIBITORS; FAMILY KINASES; DISCOVERY; GROWTH; RESISTANCE; PROTEIN; OPTIMIZATION; ACTIVATION; EXPRESSION, Saw an article supported by the WelchThe Welch Foundation [I-1829]; ACSAmerican Cancer Society [RSG-18-039-01-DMC]; Career Enhancement Grant through NIHUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USA [P50CA07090720]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Du, GY; Rao, SM; Gurbani, D; Henning, NJ; Jiang, J; Che, JW; Yang, A; Ficarro, SB; Marto, JA; Aguirre, AJ; Sorger, PK; Westover, KD; Zhang, TH; Gray, NS. The CAS is 87-63-8. Through research, I have a further understanding and discovery of 2-Chloro-6-methylaniline. Safety of 2-Chloro-6-methylaniline
SRC is a major regulator of many signaling pathways and contributes to cancer development. However, development of a selective SRC inhibitor has been challenging, and FDA-approved SRC inhibitors, dasatinib and bosutinib, are multitargeted kinase inhibitors. Here, we describe our efforts to develop a selective SRC covalent inhibitor by targeting cysteine 277 on the P-loop of SRC. Using a promiscuous covalent kinase inhibitor (CKI) SM1-71 as a starting point, we developed covalent inhibitor 15a, which discriminates SRC from other covalent targets of SM1-71 including TAK1 and FGFR1. As an irreversible covalent inhibitor, compound 15a exhibited sustained inhibition of SRC signaling both in vitro and in vivo. Moreover, 15a exhibited potent antiproliferative effects in nonsmall cell lung cancer cell lines harboring SRC activation, thus providing evidence that this approach may be promising for further drug development efforts.
About 2-Chloro-6-methylaniline, If you have any questions, you can contact Du, GY; Rao, SM; Gurbani, D; Henning, NJ; Jiang, J; Che, JW; Yang, A; Ficarro, SB; Marto, JA; Aguirre, AJ; Sorger, PK; Westover, KD; Zhang, TH; Gray, NS or concate me.. Safety of 2-Chloro-6-methylaniline
Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics