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编 号:F194188
分子式:C17H20N6O4S
分子量:404.44
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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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生物活性:
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS.

体内研究:
当与 5-FU (HY-90006) 共同处理时,Bromosporine (100 mg/kg;腹腔注射;每日一次,持续 10 天) 显示出比单独使用更好的抗肿瘤活性。Animal Model:Female BALB/c nude mice (5-6 weeks; injected with 1?×?106?cells/100?μL of HT116?cells)
Dosage:100 mg/kg
Administration:i.p.; daily for 10 days
Result:Exhibited better antitumor activity than individual Bromosporine or 5-FU (HY-90006) when co-treated with the two agent.

体外研究:
Bromosporine (0-1000 nM;72 小时) 与 5-FU(HY-90006) 协同抑制 CRC 细胞的生长 。 Bromosporine (不同浓度;48 小时) 与 5-FU 联用时导致在G1期阻滞的细胞数量明显增加。 Bromosporine (不同浓度;48 h) 降低 PARP、caspase 3 和 9 表达。 Bromosporine (0.1、0.5 和 1 μM;6-10 天) 以剂量依赖性方式抑制 AML 细胞。 Bromosporine (2.5 μM;72 小时) 在体外激活潜伏 HIV-1 J-Lat 克隆 C11 细胞中的 HIV-1 复制。 Bromosporine (1-50 μM;48 h) 不会在原代 CD4+ T 细胞中引起显著毒性。
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