产品
编 号：F753763
分子式：C23H19ClF2N8O5S
分子量：592.96
分子式：C23H19ClF2N8O5S
分子量：592.96
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 2565705-03-3
产品详情
生物活性：
Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 0.17 nM.
体内研究：
Dot1L-IN-5 (Compound 11; subcutaneous injection; at 75 mg/kg once daily for 20 days) does not lead to tumor growth inhibition in NOD-SCID mice. Dot1L-IN-5 (subcutaneous injection; at 75 mg/kg twice daily for 20 days) leads 73% growth inhibition.While both treatment regimens result in very strong inhibition of global H3K79 dimethylation level in tumor, the efficacious regimen is superior in reducing the mRNA expression of the target genes HOXA9 and MEIS1.Animal Model:NOD-SCID mice bearing subcutaneous MV4-11 tumor xenografts
Dosage:75 mg/kg
Administration:Subcutaneous injection; at 75 mg/kg once or twice daily for 20 days
Result:Once daily administration did not lead to tumor growth inhibition, 73% growth inhibition was measured in the twice daily treated group.
体外研究：
Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=30 nM).
Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 0.17 nM.
体内研究：
Dot1L-IN-5 (Compound 11; subcutaneous injection; at 75 mg/kg once daily for 20 days) does not lead to tumor growth inhibition in NOD-SCID mice. Dot1L-IN-5 (subcutaneous injection; at 75 mg/kg twice daily for 20 days) leads 73% growth inhibition.While both treatment regimens result in very strong inhibition of global H3K79 dimethylation level in tumor, the efficacious regimen is superior in reducing the mRNA expression of the target genes HOXA9 and MEIS1.Animal Model:NOD-SCID mice bearing subcutaneous MV4-11 tumor xenografts
Dosage:75 mg/kg
Administration:Subcutaneous injection; at 75 mg/kg once or twice daily for 20 days
Result:Once daily administration did not lead to tumor growth inhibition, 73% growth inhibition was measured in the twice daily treated group.
体外研究：
Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=30 nM).
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