Eprenetapopt (APR-246)

For research use only.

Catalog No.S7724 Synonyms: PRIMA-1MET

2 publications

Eprenetapopt (APR-246) Chemical Structure

CAS No. 5291-32-7

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.

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Selleck's Eprenetapopt (APR-246) has been cited by 2 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.
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 MXvD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M3yycohq\2hic3Xud4l1cX[rdImgZY5lKGOnbHyg[IVifGhiaX7keYN1cW:wIHnuJIFtdCCWUEWzcZV1KGyndXvlcYlieyxiYoX0JIxwfyCDUGKtNlQ3KHOnboPpeIl3cXS7IHnuJHRRPTO5dDDBUGw> M1\XblMyODd|MEe2
UoCB-6 M1vZe2NmdGxidnnhZoltcXS7IHHzd4F6 MlG1bIlocCC|ZX7zbZRqfmm2eTDhcoQh[2WubDDk[YF1cCCrbnT1Z5Rqd25iaX6gZYxtKFSSNUPteZQhdGW3a3XtbYF{NCCkdYSgcI94KEGSUj2yOFYhe2Wwc3n0bZZqfHliaX6gWHA2O3e2IFHMUC=> MkX3N|ExPzNyN{[=
EU-3 NW[0VFdvS2WubDD2bYFjcWyrdImgZZN{[Xl? MVLobYdpKHOnboPpeIl3cXS7IHHu[EBk\WyuIHTlZZRpKGmwZIXjeIlwdiCrbjDhcIwhXFB3M331eEBt\XWtZX3pZZMtKGK3dDDsc5chSVCULUK0OkB{\W6|aYTpeol1gSCrbjDUVFU{f3RiQVzM MWOzNVA4OzB5Nh?=
MUTZ-5 NETtZ21E\WyuII\pZYJqdGm2eTDhd5NigQ>? MX\obYdpKHOnboPpeIl3cXS7IHHu[EBk\WyuIHTlZZRpKGmwZIXjeIlwdiCrbjDhcIwhXFB3M331eEBt\XWtZX3pZZMtKGK3dDDsc5chSVCULUK0OkB{\W6|aYTpeol1gSCrbjDUVFU{f3RiQVzM M3W2WFMyODd|MEe2
KOPN-8 M3GzWGNmdGxidnnhZoltcXS7IHHzd4F6 NEDOOnBpcWeqIIPlcpNqfGm4aYT5JIFv\CClZXzsJIRm[XSqIHnu[JVkfGmxbjDpckBidGxiVGC1N412fCCuZYXr[Y1q[XNuIHL1eEBtd3diQWDSMVI1PiC|ZX7zbZRqfmm2eTDpckBVWDV|d4SgRWxN MnPjN|ExPzNyN{[=
RS4;11 Mo\CR4VtdCC4aXHibYxqfHliYYPzZZk> NWTBcoVRcGmpaDDz[Y5{cXSrdnn0fUBidmRiY3XscEBl\WG2aDDpcoR2[3Srb36gbY4h[WyuIGTQOVNufXRibHX1b4VucWG|LDDieZQhdG:5IFHQVk0zPDZic3Xud4l1cX[rdImgbY4hXFB3M4f0JGFNVA>? NFLUVWM{OTB5M{C3Oi=>
SKBR3 NWi0OIc4S2WubDDjfYNt\SCjc4PhfS=> NFvZRZY2KML3TR?= MYWyJJdm\Wu| MYfsZZBifGmwaXKgbY4h[2:vYnnuZZRqd25id3n0bEBCWFJvMkS2JINifXOnZDDhJIxwf2W{IHzleoVtKG:oIFexJIFzemW|dDDhcoQh[W5iaX7jdoVie2ViaX6geIhmKHO3Yj3HNUBnemGldHnvci=> MYCzNFc1Ozl7Nh?=
BT549 MXTD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MmHtTWM2OD1|LkGg{txO NIP3TpA{ODF7NkKzOi=>
MDA-MB-468 NWTQRnk3S2WubDD2bYFjcWyrdImgZZN{[Xl? NXLuRmJQUUN3ME21JO69VQ>? Mo\nN|AyQTZ{M{[=
MDA-MB-231 MlXzR4VtdCC4aXHibYxqfHliYYPzZZk> NVfLeGdCUUN3ME20MlEh|ryP MlfXN|AyQTZ{M{[=
HCC1143 NXLXfIhXS2WubDD2bYFjcWyrdImgZZN{[Xl? MlfLTWM2OD14Lkig{txO NFvEcGM{ODF7NkKzOi=>
MDA-MB-453 M{e3emNmdGxidnnhZoltcXS7IHHzd4F6 MX3JR|UxRTBwOTFOwG0> MXSzNFE6PjJ|Nh?=
UMSCC10A Mo\xR4VtdCC4aXHibYxqfHliYYPzZZk> Mmj5NE02OCEQvF2= M1fP[lczKGh? NFS4b|d{fXCycnXzd4VlKGOnbHygd5Vzfmm4YXygZY5lKGKxcnWgZUBud2Snc4Sg[YZn\WO2IH;uJJRp\SCtaXzsbY5oKG:oIFjOV2NEKGOnbHzz MXiyPVM1QDR4Mh?=
FaDu NI\UUXVE\WyuII\pZYJqdGm2eTDhd5NigQ>? M2K5XVAuPTBizszN MkCzO|IhcA>? M2m3XZN2eHC{ZYPz[YQh[2WubDDzeZJ3cX[jbDDhcoQh[m:{ZTDhJI1w\GW|dDDl[oZm[3Rib36geIhmKGurbHzpcochd2ZiSF7TR2Mh[2WubIO= M2P3bFI6OzR6NE[y

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
FL-PARP / Cleaved PARP ; 

PubMed: 26452133     

PARP cleavage was detected by western blotting analysis after treated with PRIMA-1(met) at different concentrations for 24 hours. 


PubMed: 26452133     

Phosphorylation of p53 level was determined after PRIMA-1(met) treatment.

Growth inhibition assay
Cell viability; 

PubMed: 26452133     

A panel of CRC cell lines was treated with either DMSO control or PRIMA-1(met) at indicated dosages for 48 hours, followed by CTG assays. The percentage of cell growth inhibition was normalized with respective DMSO control. 

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].


Cell Research:


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  • 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. 

    (Only for Reference)
Animal Research:


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  • Animal Models: CD-1 Nu/Nu mice
  • Dosages: 400 mg/kg/day
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (200.75 mM)
Water 40 mg/mL (200.75 mM)
Ethanol '40 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 199.25


CAS No. 5291-32-7
Storage powder
in solvent
Synonyms PRIMA-1MET
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 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID