M4205 (M-4205) is a highly selective inhibitor of disease-relevant cKIT mutations for unresectable metastatic or recurrent gastrointestinal stromal tumors (GIST). It had high activity against exon 11, 13 and 17 mutations of cKIT, with high kinase selectivity, with excellent metabolic stability, permeability, and solubility. Preclinical studies of M4205 in GIST xenograft models expressing mutations in exon 11 showed that M4205 delivered strong responses compared with imatinib. Compared with second-line standard of care sunitinib, M4205 treatment resulted in deeper anti-tumor response in xenograft models expressing secondary resistance mutations in exon 13. Similar results were seen in a xenograft model expressing secondary resistance mutations in exon 17. M4205 has the potential to become a best-in-class option for GIST. There is a phase I clinical study of GIST in preparation.

纯度：≥98%

CAS：2590556-80-0