PAB 0099 | Quizartinib; AC-010220; AC-220 | Quizartinib yog ib qho inhibitor ntawm FMS-txog tyrosine kinase 3 (FLT3; Kd = 1.6 nM) thiab ua kom pom kev xaiv siab rau FLT3 thaum kuaj tawm tsam ntawm 227 kinases ntxiv. Nws inhibits qhov kev loj hlob ntawm tib neeg leukemia cell kab MV4-11, uas harbors ib homozygous FLT3-ITD kev hloov, nrog rau IC50 tus nqi ntawm 0.56 nM.1 Ntawm 1 mg / kg / hnub, quizartinib tau pom tias kom muaj sia nyob ntev hauv nas. Tus qauv ntawm FLT3-ITD mob myeloid leukemia thiab tshem tawm cov qog hauv ib qho FLT3-dependent nas xenograft qauv ntawm 10 mg/kg. |