Application of 3235-67-4. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1-Piperidineacetic Acid, is researched, Molecular C7H13NO2, CAS is 3235-67-4, about Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I “”Gatekeeper”” Mutant of cKIT Kinase. Author is Li, Binhua; Wang, Aoli; Liu, Juan; Qi, Ziping; Liu, Xiaochuan; Yu, Kailin; Wu, Hong; Chen, Cheng; Hu, Chen; Wang, Wenchao; Wu, Jiaxin; Hu, Zhenquan; Ye, Ling; Zou, Fengming; Liu, Feiyang; Wang, Beilei; Wang, Li; Ren, Tao; Zhang, Shaojuan; Bai, Mingfeng; Zhang, Shanchun; Liu, Jing; Liu, Qingsong.
CKIT kinase inhibitors, e.g., imatinib could induce drug-acquired mutations such as cKIT T670I that rendered drug resistance after chronic treatment. Through a type II kinase inhibitor design approach the authors discovered a highly potent type II cKIT kinase inhibitor compound 35 (CHMFL-KIT-8140), which potently inhibited both cKIT wt (IC50: 33 nM) and cKIT gatekeeper T670I mutant (IC50: 99 nM). Compound 35 displayed strong anti-proliferative effect against GISTs cancer cell lines GIST-T1 (cKIT wt, GI50: 4 nM) and GIST-5R (cKIT T670I, GI50: 26 nM). In the cellular context it strongly inhibited c-KIT mediated signaling pathways and induced apoptosis. In the BaF3-TEL-cKIT-T670I isogenic cell inoculated xenograft mouse model, 35 exhibited dose dependent tumor growth suppression efficacy and 100 mg/kg dosage provided 47.7% tumor growth inhibition (TGI) without obvious toxicity. The authors believe compound 35 would be a good pharmacol. tool for exploration of the cKIT-T670I mutant mediated pathol. in GISTs.
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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem