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)
10mg	电议
25mg	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，IC50 SPA DOT1L 为 0.17 nM。

Cas No.

2565705-03-3

分子式

C₂₃H₁₉ClF₂N₈O₅S

分子量

592.96

溶解度

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

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

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

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].

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.