1. Epigenetics
  2. Histone Methyltransferase
  3. Dot1L-IN-5

Dot1L-IN-5 是一种有效的类端粒沉默干扰体 1 (DOT1L) 抑制剂,IC50 为 0.17 nM。

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Dot1L-IN-5 Chemical Structure

Dot1L-IN-5 Chemical Structure

CAS No. : 2565705-03-3

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥3520
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1 mg ¥1454
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5 mg ¥3200
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10 mg ¥5440
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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 (ED50 H3K79me2 Elisa=2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=30 nM)[1].

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

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].

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

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

Formula

C23H19ClF2N8O5S

CAS 号
性状

固体

颜色

White to off-white

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 中的溶解度 : 250 mg/mL (421.61 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Dot1L-IN-5 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6865 mL 8.4323 mL 16.8645 mL 42.1614 mL
5 mM 0.3373 mL 1.6865 mL 3.3729 mL 8.4323 mL
10 mM 0.1686 mL 0.8432 mL 1.6865 mL 4.2161 mL
15 mM 0.1124 mL 0.5622 mL 1.1243 mL 2.8108 mL
20 mM 0.0843 mL 0.4216 mL 0.8432 mL 2.1081 mL
25 mM 0.0675 mL 0.3373 mL 0.6746 mL 1.6865 mL
30 mM 0.0562 mL 0.2811 mL 0.5622 mL 1.4054 mL
40 mM 0.0422 mL 0.2108 mL 0.4216 mL 1.0540 mL
50 mM 0.0337 mL 0.1686 mL 0.3373 mL 0.8432 mL
60 mM 0.0281 mL 0.1405 mL 0.2811 mL 0.7027 mL
80 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5270 mL
100 mM 0.0169 mL 0.0843 mL 0.1686 mL 0.4216 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

产品名称:
Dot1L-IN-5
目录号:
HY-135128
需求量: