Dot1L-IN-4|cas:2565705-02-2|西域试剂

Dot1L-IN-4,99.60%

产品编号：Bellancom-135127| CAS NO：2565705-02-2| 分子式：C₂₈H₂₇ClF₂N₈O₅S| 分子量：661.08

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-135127	￥4500.00	杭州北京（现货）
Bellancom-135127	￥7600.00	杭州北京（现货）
Bellancom-135127	￥14000.00	杭州北京（现货）

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Dot1L-IN-4

产品介绍

Dot1L-IN-4 是一种有效的类端粒沉默干扰体 1 (DOT1L) 抑制剂，IC_{50 SPA DOT1L} 为 0.11 nM。

生物活性

Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC_{50 SPA DOT1L} of 0.11 nM.

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 (ED_{50 H3K79me2 Elisa}=1.7 nM) and HOXA9 gene expression in Molm-13 cells (ED_{50 HOXA9 RGA}=33 nM). Dot1L-IN-4 also inhibits mixed lineage leukemia (MLL) with an IC₅₀ of 99 µM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 220 mg/mL (332.79 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5127 mL	7.5634 mL	15.1268 mL
5 mM	0.3025 mL	1.5127 mL	3.0254 mL
10 mM	0.1513 mL	0.7563 mL	1.5127 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (3.15 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (3.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。