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编 号:F246477
分子式:C42H50FN7O8S2
分子量:864.02
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.

体内研究:
Bomedemstat treatment (oral gavage; 45?mg/kg; once daily; 56 d) normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis.Animal Model:Mx-Jak2V617F mice
Dosage:45?mg/kg
Administration:Oral gavage; 45?mg/kg; once daily; 56 days
Result:Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.

体外研究:
Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2V617F cells by concomitantly increasing expression and methylation of p53.Bomedemstat (50 nM-1 μM; 96 h) enhances survival, induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, and leads to cell cycle arrest.
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