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

Abexinostat  (Synonyms: CRA 024781; PCI-24781)

Cat. No.: HY-10990 Purity: 98.11%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Abexinostat Chemical Structure

Abexinostat Chemical Structure

CAS No. : 783355-60-2

Size Price Stock Quantity
1 mg USD 43 In-stock
5 mg USD 92 In-stock
10 mg USD 145 In-stock
50 mg USD 462 In-stock
100 mg USD 726 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

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)

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].

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

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].

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

Clinical Trial
Molecular Weight

397.42

Formula

C21H23N3O5

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NCCOC1=CC=C(C=C1)C(NO)=O)C2=C(C3=CC=CC=C3O2)CN(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (8.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  20% HP-β-CD in Saline

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.61%

References
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.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 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
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Abexinostat Related Classifications

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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Product Name:
Abexinostat
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HY-10990
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