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编 号:F711984
分子式:C23H30Cl2N2O2
分子量:437.4
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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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50mg
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100mg
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生物活性:
GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.

体内研究:
GSK2879552 dihydrochloride (1.5 mg/kg,po) 处理在携带 SCLC 异种移植物的小鼠中表现出肿瘤生长抑制。Animal Model:NCI-H526 and NCI-H1417 xenografts.
Dosage:1.5 mg/kg.
Administration:PO daily for 25-35 days.
Result:There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.

体外研究:
GSK2879552 dihydrochloride 抑制 KDM1A 组蛋白去甲基化酶活性,诱导索拉非尼耐药细胞的分化并减弱干细胞特性。GSK2879552 dihydrochloride 在索拉非尼耐药细胞中抑制 Wnt 拮抗剂的转录并下调 β-catenin 信号活性。
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