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  2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. Abexinostat

Abexinostat  (Synonyms: 阿貝司他; 艾貝司他; CRA 024781; PCI-24781)

目錄號(hào): HY-10990 純度: 98.63%
COA 產(chǎn)品使用指南

Abexinostat (CRA 024781) 是一種新的泛 HDAC 抑制劑，主要靶向 HDAC1 的 Ki 值為 7 nM。Abexinostat 也抑制 MBLAC2 水解酶活性，EC50 小于 10 nM。

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Abexinostat Chemical Structure

Abexinostat Chemical Structure

CAS No. : 783355-60-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥350
In-stock
5 mg ￥800
In-stock
10 mg ￥1200
In-stock
50 mg ￥3800
In-stock
100 mg ￥6000
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM. Abexinostat also inhibits metallo-β-lactamase domain-containing protein?2 (MBLAC2) hydrolase activity with an EC50 below 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)

體外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)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].

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

397.42

Formula

C21H23N3O5
CAS 號(hào)
性狀

固體

顏色

Off-white to pink

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 3.33 mg/mL (8.38 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5162 mL 12.5811 mL 25.1623 mL
5 mM 0.5032 mL 2.5162 mL 5.0325 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑： 20% HP-β-CD in Saline

    Solubility: 6 mg/mL (15.10 mM); 懸濁液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.63%

參考文獻(xiàn)
Cell Assay
[1]

Ten tumor cell lines and HUVEC are cultured for at least two doubling times, and growth is monitored at the end of compound exposure using an Alamar blue fluorometric cell proliferation assay. The compound is assayed in triplicate wells in 96-well plates at nine concentrations using half-log intervals ranging from 0.0015 to 10 μmol/L. The final DMSO concentration in each well is 0.15%. The concentration required to inhibit cell growth by 50% and 95% confidence intervals are estimated from nonlinear regression using a four-parameter logistic equation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

HCT116 and DLD-1 tumor cells are implanted s.c. in female BALB/c nu/nu mice at 3×106 per mouse. Treatment with Abexinostat (CRA 024781) started when the average tumor volume is -100 mm[1]. Mice bearing human colon tumor xenografts are dosed i.v. with Abexinostat (CRA 024781) using various dosages and schedules to assess the antitumor activity of Abexinostat (CRA 024781) [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5162 mL 12.5811 mL 25.1623 mL 62.9057 mL
5 mM 0.5032 mL 2.5162 mL 5.0325 mL 12.5811 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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產(chǎn)品名稱：
Abexinostat
目錄號(hào)：
HY-10990
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