产品
编 号:F282812
分子式:C11H9F3N4O2S
分子量:318.27
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10mM*1mL in DMSO
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1mg
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5mg
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生物活性:
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 μM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.

体内研究:
BRM/BRG1 ATP Inhibitor-1 (化合物14) (口服,7.5或20 mg/kg,每天,3周) 可抑制肿瘤生长,并呈剂量依赖性抑制KRT80表达。Animal Model:Female athymic nude mice with RERF-LC-AI tumor xenografts
Dosage:7.5 mg/kg, 20 mg/kg
Administration:Oral administration; everyday; 3 weeks
Result:Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively.Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.

体外研究:
BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM,5 days) 可以抑制癌细胞的增殖。 BRM/BRG1 ATP Inhibitor-1 抑制 KRT80 基因的表达,在 H1299 细胞中的 AAC50 (绝对 AC50) 值为 0.01 μM,在 RERF-LC-AI 细胞中的 AAC50 为 0.01 μM。
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