X-376 is identified as a highly potent and specific inhibitor of the ALK tyrosine kinase (TKI), boasting an IC50 value of 0.61 nM, making it less effective against MET with an IC50 of 0.69 nM. Its anticancer efficacy is pronounced[1].
X-376 动物研究
Animal study
In vivo, X-376 demonstrates notable antitumor activity in H3122 xenograft models, featuring significant bioavailability and moderate half-lives. When administered at 50 mg/kg bid to nude mice with H3122 xenografts, it considerably slows tumor growth compared to control, without affecting mouse weight or showing signs of compound-related toxicity. Further safety assessments in Sprague Dawley (SD) rats, with doses up to 100 mg/kg following 10 days of repeated oral administration, show survival without significant toxicity. The determined no significant toxicity (NST) level for X-376 is at 50 mg/kg, achieving an AUC of 41 μM×hr and a Cmax of 5.04 μM[1].
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