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Abexinostat
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。
Abexinostat图片
CAS NO:783355-60-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
阿贝司他
艾贝司他
CRA 024781
PCI-24781
产品介绍
Abexinostat (CRA 024781) 是一种新的泛HDAC抑制剂,主要靶向 HDAC1 的Ki值为 7 nM。Abexinostat 也抑制MBLAC2水解酶活性,EC50小于 10 nM。
生物活性

Abexinostat (CRA 024781) is a novel pan-HDACinhibitor mostly targetingHDAC1withKiof 7 nM. Abexinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with anEC50below 10 nM[1][4].

IC50& Target[1][4]

HDAC1

7 nM (Ki)

HDAC3/SMRT

8.2 nM (Ki)

HDAC6

17 nM (Ki)

HDAC2

19 nM (Ki)

HDAC10

24 nM (Ki)

HDAC8

280 nM (Ki)

MBLAC2

<10 nM (EC50)

体外研究
(In Vitro)

Abexinostat (CRA 024781) exhibits potent antitumor activity against a variety of tumor cell lines with GI50%ranging from 0.15 μM to 3.09 μM. Abexinostat (CRA 024781) also has an antiproliferative effect on HUVEC endothelial cells with GI50%of 0.43 μM. Abexinostat (CRA 024781) treatment causes dose-dependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells, induces expression of p21, and leads to PARP cleavage and accumulation of the γH2AX[1]. Inhibition of HDAC enzymes by Abexinostat (CRA 024781) leads to a significant reduction in the transcription of genes specifically associated with HR, including RAD51. Consistent with inhibition of HR, Abexinostat (CRA 024781) treatment results in a decreased ability to perform homology directed repair of I-SceI-induced chromosome breaks in transfected CHO cells[2]. Abexinostat (CRA 024781) induces S phase depletion, G2 cell cycle arrest, and apoptosis in soft tissue sarcoma (STS) cells. Abexinostat (CRA 024781) induces Rad51 transcriptional repression in STS cells potentially mediated via enhanced E2F1 binding to the Rad51 proximal promoter[3].

体内研究
(In Vivo)

Abexinostat (CRA 024781) parenterally administered to mice harboring HCT116 or DLD-1 colon tumor xenografts results in a statistically significant reduction in tumor growth. Inhibition of tumor growth is accompanied by an increase in the acetylation of α-tubulin in peripheral blood mononuclear cells, and an alteration in the expression of many genes in the tumors, including several involved in apoptosis and cell growth[1].

Clinical Trial
分子量

397.42

性状

Solid

Formula

C21H23N3O5

CAS 号

783355-60-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

溶解性数据
In Vitro: 

DMSO : 3.33 mg/mL(8.38 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5162 mL12.5811 mL25.1623 mL
5 mM0.5032 mL2.5162 mL5.0325 mL
10 mM---------
*

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;该产品在溶液状态不稳定,建议您现用现配,即刻使用

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: 20%HP-β-CDin saline

    Solubility: 6 mg/mL (15.10 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。