Abexinostat
Based on 9 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.00%
- CAS 番号: 783355-60-2
- 分子式: C21H23N3O5
- 分子量:397.42
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保管条件:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Abexinostat
More- Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]
- Cell Rep. 2024 May 24;43(6):114272. [Abstract]
- Viruses. 2020 Jun 3;12(6):609. [Abstract]
- Int J Parasitol Drugs Drug Resist. 2026 May 17;31:100649.
- bioRxiv. 2025 Aug 25.
- Patent. US20250161243A1.
- Research Square Print. 2023 Mar 9.
- bioRxiv. 2021 Jan 5.
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
生物活性
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AML12 | IC50 |
1.82 μM
Compound: Abexinostat
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Cytotoxicity against AML12 cells incubated for 72 hrs measured by MTT assay
Cytotoxicity against AML12 cells incubated for 72 hrs measured by MTT assay
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[PMID: 37498552] |
| Bel-7402 | IC50 |
0.37 μM
Compound: Abexinostat
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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
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[PMID: 37498552] |
| HepG2 | IC50 |
0.21 μM
Compound: Abexinostat
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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
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[PMID: 37498552] |
| Huh-7 | IC50 |
1.01 μM
Compound: Abexinostat
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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
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[PMID: 37498552] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 783355-60-2
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性状 Solid
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分子量 397.42
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分子式 C21H23N3O5
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Color Off-white to pink
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SMILES
O=C(NCCOC1=CC=C(C=C1)C(NO)=O)C2=C(C3=CC=CC=C3O2)CN(C)C
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別名
CRA 024781; PCI-24781
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (9)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431
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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Cell Rep
Decrypting lysine deacetylase inhibitor action and protein modifications by dose-resolved proteomics. [Abstract]2024 May 24;43(6):114272. PMID: 38795348 -
Viruses
Identification of Combinations of Protein Kinase C Activators and Histone Deacetylase Inhibitors That Potently Reactivate Latent HIV. [Abstract]2020 Jun 3;12(6):609. PMID: 32503121 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
溶剤 & 溶解度
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)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 20% HP-β-CD in Saline
Solubility: 6 mg/mL (15.10 mM); Suspended solution; Need ultrasonic
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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 |
| 5 mM | 0.5032 mL | 2.5162 mL | 5.0325 mL | 12.5811 mL |
Abexinostat 関連分類
HY-10990 関連分類
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