Dot1L-IN-5

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Dot1L-IN-5

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2565705-03-3

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

Dot1L-IN-5 是一种有效的类端粒沉默干扰体 1 (DOT1L) 抑制剂，IC_{50 SPA DOT1L}为 0.17 nM。

生物活性

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with anIC_{50 SPADOT1L}of 0.17 nM^[1].

IC₅₀& Target^[1]

DOT1L

0.17 nM (IC₅₀)

体外研究
(In Vitro)

Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED_{50 H3K79me2 Elisa}=2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED_{50 HOXA9 RGA}=30 nM)^[1].

体内研究
(In Vivo)

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^[1].
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^[1].

Animal Model:	NOD-SCID mice bearing subcutaneous MV4-11 tumor xenografts^[1]
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.

分子量

592.96

性状

Solid

Formula

C₂₃H₁₉ClF₂N₈O₅S

CAS 号

2565705-03-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 250 mg/mL(421.61 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.6865 mL	8.4323 mL	16.8645 mL
5 mM	0.3373 mL	1.6865 mL	3.3729 mL
10 mM	0.1686 mL	0.8432 mL	1.6865 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。