1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. CRA-026440

CRA-026440 是一种有效的广谱 HDAC 抑制剂。作用于 HDAC1HDAC2HDAC3HDAC6HDAC8HDAC10Ki 分别为 4,14,11,15,7 和 20 nM。CRA-026440 具有抗肿瘤和抗血管生成活性。

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CRA-026440 Chemical Structure

CRA-026440 Chemical Structure

CAS No. : 847460-34-8

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规格 是否有货
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100 mg   询价  
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CRA-026440 的其他形式现货产品:

Other Forms of CRA-026440:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities[1]. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

HDAC1

4 nM (Ki)

HDAC8

7 nM (Ki)

HDAC3

11 nM (Ki)

HDAC2

14 nM (Ki)

HDAC6

15 nM (Ki)

HDAC10

20 nM (Ki)

体外研究
(In Vitro)

CRA-026440 对 HUVEC 内皮细胞具有抗增殖作用,GI50 值为 1.41 μM[1]
CRA-026440(0.1-10 μM;18 小时)导致乙酰化组蛋白和乙酰化微管蛋白的积累,从而抑制肿瘤细胞生长并诱导细胞凋亡[1]
CRA-026440(0.1-10 μM;5 天)以剂量依赖性方式抑制离体血管生成[1]

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

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM
Incubation Time: 18 hours
Result: Resulted in the accumulation of both acetylated histones and acetylated tubulin. Induced expression of the cyclin-dependent kinase inhibitor p21Cip1/WAF1.
体内研究
(In Vivo)

CRA-026440(100 mg/kg;静脉注射;每天;连续三天)导致携带 HCT116 或 U937 人肿瘤异种移植物的小鼠肿瘤生长显着减少[1]

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

Animal Model: HCT-116 tumor-bearing nude mice[1]
Dosage: 100 mg/kg
Administration: i.v.; daily; for three consecutive days
Result: Resulted in a statistically significant reduction in tumor growth.
分子量

420.46

Formula

C23H24N4O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (237.83 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 2.3783 mL 11.8917 mL 23.7835 mL
5 mM 0.4757 mL 2.3783 mL 4.7567 mL
查看完整储备液配制表
  • 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

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3783 mL 11.8917 mL 23.7835 mL 59.4587 mL
5 mM 0.4757 mL 2.3783 mL 4.7567 mL 11.8917 mL
10 mM 0.2378 mL 1.1892 mL 2.3783 mL 5.9459 mL
15 mM 0.1586 mL 0.7928 mL 1.5856 mL 3.9639 mL
20 mM 0.1189 mL 0.5946 mL 1.1892 mL 2.9729 mL
25 mM 0.0951 mL 0.4757 mL 0.9513 mL 2.3783 mL
30 mM 0.0793 mL 0.3964 mL 0.7928 mL 1.9820 mL
40 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4865 mL
50 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1892 mL
60 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9910 mL
80 mM 0.0297 mL 0.1486 mL 0.2973 mL 0.7432 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5946 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:
CRA-026440
目录号:
HY-19754
需求量: