货号	规格	价格	上海	北京	珠海	重庆	武汉
S89290-5mg	98.60%	￥750.00 S89290-5mg ￥750.00 现货	6 6	-	-	-	-
S89290-10mg	98.60%	￥1200.00 S89290-10mg ￥1200.00 现货	6 6	-	-	-	-
S89290-25mg	98.60%	￥2250.00 S89290-25mg ￥2250.00 现货	5 5	-	-	-	-
S89290-100mg	≥98%	￥6000.00 S89290-100mg ￥6000.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM

靶点：

DOT1L:0.11 nM (IC50);HistoneMethyltransferase

体外研究：

Dot1L-IN-4 (Compound 10) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=1.7 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=33 nM). Dot1L-IN-4 also inhibits mixed lineage leukemia (MLL) with an IC50 of 99 µM.

体内研究：

Dot1L-IN-4 (Compound 10; 300 mg/kg; p.o.; qd) is not tolerated at such a high dose by tumor xenograft bearing mice, and at a 6-fold reduced dose, the tumor growth as well as the HOXA9 reporter gene mRNA are reduced only by less than half as compared to control animals. Animal Model: Male mice (C57BL/6) bearing subcutaneous MV4-11 tumor xenografts Dosage: 300 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Was not tolerated at such a high dose by tumor xenograft bearing mice, and at a 6-fold reduced dose, the tumor growth as well as the HOXA9 reporter gene mRNA were reduced only by less than half as compared to control animals.

参考文献：

1. Frédéric Stauffer, et al. New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse. ACS Med. Chem. Lett. 2019, 10, 12, 1655-1660.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.513 ml	7.563 ml	15.127 ml
5 mM	0.303 ml	1.513 ml	3.025 ml
10 mM	0.151 ml	0.756 ml	1.513 ml
50 mM	0.03 ml	0.151 ml	0.303 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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