产品
编 号：F757705
分子式：C18H16N2O2
分子量：292.33
分子式：C18H16N2O2
分子量：292.33
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 353495-21-3
产品详情
生物活性：
BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM.
体内研究：
BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice.Animal Model:NSGS mice, K562 (ASXL1-WT/Y591*) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588*) model
Dosage:50 mg/kg/d
Administration:Intraperitoneal injection, drug treatments were started at day 28 after transplantation
Result:Significantly delayed progression of disease in both models.
体外研究：
BAP1-IN-1 (Compound 8) (1 μM; 30 min) specifically inhibits BAP1 not just in vitro but also within the cellular context.BAP1-IN-1 (0.1 μM; 24 h) significantly alters 240 genes in BAP1-WT cells, whereas only 33 transcripts are changed in BAP1-KO cells, demonstrating that the gene expression changes mainly depend on the presence of BAP1 protein.BAP1-IN-1 (0-10 μM; 72 h) selectively inhibits cells with ASXL1 GOF mutations.
BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM.
体内研究：
BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice.Animal Model:NSGS mice, K562 (ASXL1-WT/Y591*) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588*) model
Dosage:50 mg/kg/d
Administration:Intraperitoneal injection, drug treatments were started at day 28 after transplantation
Result:Significantly delayed progression of disease in both models.
体外研究：
BAP1-IN-1 (Compound 8) (1 μM; 30 min) specifically inhibits BAP1 not just in vitro but also within the cellular context.BAP1-IN-1 (0.1 μM; 24 h) significantly alters 240 genes in BAP1-WT cells, whereas only 33 transcripts are changed in BAP1-KO cells, demonstrating that the gene expression changes mainly depend on the presence of BAP1 protein.BAP1-IN-1 (0-10 μM; 72 h) selectively inhibits cells with ASXL1 GOF mutations.
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