Eprenetapopt (APR-246)

Catalog No.S7724 Synonyms: PRIMA-1MET

For research use only.

Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.

Eprenetapopt (APR-246) Chemical Structure

CAS No. 5291-32-7

Selleck's Eprenetapopt (APR-246) has been cited by 9 Publications

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Biological Activity

Description Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
Targets
Mutant p53 [2]
In vitro

APR-246 (PRIMA-1MET) is the first clinical-stage compound that reactivates mutant p53 and induces apoptosis. APR-246 is a prodrug that is converted to the active compound methylene quinuclidinone (MQ), a Michael acceptor that binds to cysteine residues in mutant p53 and restores its wild-type conformation. APR-246 completely restores the cisplatin and doxorubicin sensitivity to p53-mutant drug-resistant ovarian cancer cells. It not only reactivates p53 but also decreases intracellular glutathione levels in a dose-dependent manner. APR-246 can trigger apoptosis in a p53-independent manner by inducing ROS and endoplasmic reticulum (ER) stress and by inhibiting thioredoxin reductase 1 (TrxR1). It was also reported that APR-246 induces cell death in myeloma cells independently of p53 status by impairing the GSH/ROS balance[1]. PRIMA-1Met/APR-246 efficiently inhibited the growth of the SCLC cell lines expressing mutant p53 in vitro and induced apoptosis, associated with increased fraction of cells with fragmented DNA, caspase-3 activation, PARP cleavage, Bax and Noxa upregulation and Bcl-2 downregulation in the cells[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NALM-6 M2HSW2NmdGxidnnhZoltcXS7IHHzd4F6 NYXDTXprcGmpaDDz[Y5{cXSrdnn0fUBidmRiY3XscEBl\WG2aDDpcoR2[3Srb36gbY4h[WyuIGTQOVNufXRibHX1b4VucWG|LDDieZQhdG:5IFHQVk0zPDZic3Xud4l1cX[rdImgbY4hXFB3M4f0JGFNVA>? NVzJSXhuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwO|MxPzZpPkOxNFc{ODd4PD;hQi=>
UoCB-6 NFrmNG5E\WyuII\pZYJqdGm2eTDhd5NigQ>? MUDobYdpKHOnboPpeIl3cXS7IHHu[EBk\WyuIHTlZZRpKGmwZIXjeIlwdiCrbjDhcIwhXFB3M331eEBt\XWtZX3pZZMtKGK3dDDsc5chSVCULUK0OkB{\W6|aYTpeol1gSCrbjDUVFU{f3RiQVzM NEPKOHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUC3N|A4Pid-M{GwO|MxPzZ:L3G+
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SK-N-MC MXLxTHRUKGG|c3H5 NUHNcVcxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NXjvRZpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Assay
Methods Test Index PMID
Western blot FL-PARP / Cleaved PARP ; p-p53 26452133
Growth inhibition assay Cell viability 26452133
In vivo APR-246 showed a good safety profile in a Phase I/II clinical dose-finding study on hematological malignancies and prostate cancer and both clinical and p53-dependent biological responses were observed. In animal studies, APR-246 is well tolerated. Single treatment with APR-246 inhibits tumor growth by 21% in mice bearing the aggressively growing A2780-CP20 tumor xenografts[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: OVCAR-3 cells
  • Concentrations: 40 μM
  • Incubation Time: 20 h
  • Method:

    OVCAR-3 cells were plated at a density of 75 000 cells per well in 3 ml of medium in 12-well plates. Next day, 2.5 ml medium was removed and cells were treated with cisplatin or APR-246 or in combination for 20 h. Next day, cells were harvested by trypsinization, washed twice and cells were stained with Annexin V and propidium iodine (PI). After staining, the samples were analyzed by LSRII flow cytometer. 

Animal Research:

[1]

  • Animal Models: CD-1 Nu/Nu mice
  • Dosages: 400 mg/kg/day
  • Administration: i.v.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 199.25
Formula

C10H17NO3

CAS No. 5291-32-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COCC1(C(=O)C2CCN1CC2)CO

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04383938 Recruiting Drug: APR-246 (eprenetapopt) + Pembrolizumab Bladder Cancer|Gastric Cancer|Non Small Cell Lung Cancer|NSCLC|Urothelial Carcinoma|Advanced Solid Tumor Aprea Therapeutics June 25 2020 Phase 1|Phase 2
NCT04214860 Active not recruiting Drug: APR-246|Drug: Venetoclax|Drug: Azacitidine Myeloid Malignancy Aprea Therapeutics December 13 2019 Phase 1
NCT03745716 Active not recruiting Drug: APR-246 + azacitidine|Drug: Azacitidine MDS Aprea Therapeutics January 11 2019 Phase 3
NCT03391050 Terminated Drug: APR-246|Drug: Dabrafenib Melanoma Aprea Therapeutics|Jules Bordet Institute January 18 2018 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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