CRA-026440

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CRA-026440

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:

847460-34-8

CRA-026440 是一种有效的广谱HDAC抑制剂。作用于HDAC1，HDAC2，HDAC3，HDAC6，HDAC8和HDAC10的K_i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。

生物活性

CRA-026440 is a potent, broad-spectrumHDACinhibitor. TheK_ivalues against recombinantHDACisoenzymesHDAC1,HDAC2,HDAC3,HDAC6,HDAC8, andHDAC10are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities^[1].

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]。

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]。

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

847460-34-8

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

In Vitro:

DMSO : 100 mg/mL(237.83 mM;Need ultrasonic)

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
10 mM	0.2378 mL	1.1892 mL	2.3783 mL