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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.
Li B, Wang A, Liu J, Qi Z, Liu X, Yu K, Wu H, Chen C, Hu C, Wang W, Wu J, Hu Z, Ye L, Zou F, Liu F, Wang B, Wang L, Ren T, Zhang S, Bai M, Zhang S, Liu J, Liu Q. Li B, et al. Among authors: bai m. J Med Chem. 2016 Sep 22;59(18):8456-72. doi: 10.1021/acs.jmedchem.6b00902. Epub 2016 Aug 30. J Med Chem. 2016. PMID: 27545040
Repurposing cabozantinib to GISTs: Overcoming multiple imatinib-resistant cKIT mutations including gatekeeper and activation loop mutants in GISTs preclinical models.
Lu T, Chen C, Wang A, Jiang Z, Qi Z, Hu Z, Hu C, Liu F, Wang W, Wu H, Wang B, Wang L, Qi S, Wu J, Wang W, Tang J, Yan H, Bai M, Liu Q, Liu J. Lu T, et al. Among authors: bai m. Cancer Lett. 2019 Apr 10;447:105-114. doi: 10.1016/j.canlet.2019.01.024. Epub 2019 Jan 24. Cancer Lett. 2019. PMID: 30684595
Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).
Liu X, Wang B, Chen C, Qi Z, Zou F, Wang J, Hu C, Wang A, Ge J, Liu Q, Yu K, Hu Z, Jiang Z, Wang W, Wang L, Wang W, Ren T, Bai M, Liu Q, Liu J. Liu X, et al. Among authors: bai m. J Med Chem. 2019 May 23;62(10):5006-5024. doi: 10.1021/acs.jmedchem.9b00176. Epub 2019 May 14. J Med Chem. 2019. PMID: 31046271
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors.
Wu Y, Wang B, Wang J, Qi S, Zou F, Qi Z, Liu F, Liu Q, Chen C, Hu C, Hu Z, Wang A, Wang L, Wang W, Ren T, Cai Y, Bai M, Liu Q, Liu J. Wu Y, et al. Among authors: bai m. J Med Chem. 2019 Jul 11;62(13):6083-6101. doi: 10.1021/acs.jmedchem.9b00280. Epub 2019 Jun 28. J Med Chem. 2019. PMID: 31250638
Axitinib overcomes multiple imatinib resistant cKIT mutations including the gatekeeper mutation T670I in gastrointestinal stromal tumors.
Liu F, Zou F, Chen C, Yu K, Liu X, Qi S, Wu J, Hu C, Hu Z, Liu J, Liu X, Wang L, Ge J, Wang W, Ren T, Bai M, Cai Y, Xiao X, Qian F, Tang J, Liu Q, Liu J. Liu F, et al. Among authors: bai m. Ther Adv Med Oncol. 2019 May 17;11:1758835919849757. doi: 10.1177/1758835919849757. eCollection 2019. Ther Adv Med Oncol. 2019. PMID: 31205508 Free PMC article.
2,644 results