Abexinostat (Synonyms: CRA 024781; PCI-24781)

Name: Abexinostat
Brand: MedChemExpress
SKU: HY-10990
Rating: 5.0 (8 reviews)

Cat. No.: HY-10990 Purity: 99.00%: Data Sheet
COA

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Handling Instructions
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Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with K_i 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.

CAS No. : 783355-60-2

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

8 Publications Citing Use of MCE Abexinostat

Cell Proliferation/Viability Assay

: Abexinostat purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]; Immunoblotting of the indicated proteins in OVCA433 cells treated with Entinostat, Mocetinostat, or Abexinostat (0.1, 1, 10 μM).

: Abexinostat purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]; Cell viability detection at an absorbance of 450 nm in OVCA433 and A2780 cells treated with DMSO, Entinostat, Mocetinostat, or Abexinostat either alone or together with PaTrin-2 after the administration of CBP.

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View All Isoforms

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

Cellular Effect

Cell Line	Type	Value	Description	References
AML12	IC₅₀	1.82 μM Compound: Abexinostat	Cytotoxicity against AML12 cells incubated for 72 hrs measured by MTT assay Cytotoxicity against AML12 cells incubated for 72 hrs measured by MTT assay	[PMID: 37498552]
Bel-7402	IC₅₀	0.37 μM Compound: Abexinostat	Cytotoxicity against human Bel-7402 cells incubated for 72 hrs measured by MTT assay Cytotoxicity against human Bel-7402 cells incubated for 72 hrs measured by MTT assay	[PMID: 37498552]
HepG2	IC₅₀	0.21 μM Compound: Abexinostat	Cytotoxicity against human HepG2 cells incubated for 72 hrs measured by MTT assay Cytotoxicity against human HepG2 cells incubated for 72 hrs measured by MTT assay	[PMID: 37498552]
Huh-7	IC₅₀	1.01 μM Compound: Abexinostat	Cytotoxicity against human Huh-7 cells incubated for 72 hrs measured by MTT assay Cytotoxicity against human Huh-7 cells incubated for 72 hrs measured by MTT assay	[PMID: 37498552]

In Vitro

Abexinostat (CRA 024781) exhibits potent antitumor activity against a variety of tumor cell lines with GI_50% ranging from 0.15 μM to 3.09 μM. Abexinostat (CRA 024781) also has an antiproliferative effect on HUVEC endothelial cells with GI_50% 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.

783355-60-2

Appearance

Solid

Color

Off-white to pink

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
10 mM	---	---	---

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.00%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (246 KB) RP-HPLC (221 KB)

Handling Instructions (2659 KB)

References

[1]. Buggy JJ, et al. CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Mol Cancer Ther, 2006, 5(5), 1309-1317. [Content Brief]

[2]. Adimoolam S, et al. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci U S A, 2007, 104(49), 19482-19487. [Content Brief]

[3]. Lopez G, et al. Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma. Clin Cancer Res, 2009, 15(10), 3472-3483. [Content Brief]

[4]. Lechner S, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Aug;18(8):812-820. [Content Brief]

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	[1]. Buggy JJ, et al. CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Mol Cancer Ther, 2006, 5(5), 1309-1317. [Content Brief] [2]. Adimoolam S, et al. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci U S A, 2007, 104(49), 19482-19487. [Content Brief] [3]. Lopez G, et al. Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma. Clin Cancer Res, 2009, 15(10), 3472-3483. [Content Brief] [4]. Lechner S, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Aug;18(8):812-820. [Content Brief]

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
DMSO	5 mM	0.5032 mL	2.5162 mL	5.0325 mL	12.5811 mL

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.

Keywords:

Abexinostat783355-60-2CRA 024781 PCI-24781CRA024781CRA-024781PCI24781PCI 24781PCI-24781HDACHistone deacetylasesMBLAC2antitumor activityInhibitorinhibitorinhibit

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Abexinostat (Synonyms: CRA 024781; PCI-24781)

Customer Review

Abexinostat Related Antibodies

8 Publications Citing Use of MCE Abexinostat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HDAC Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Abexinostat Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Abexinostat Related Classifications

Keywords:

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Customer Review

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