APR-246 (PRIMA-1MET)

Catalog No.S7724

APR-246 (PRIMA-1MET) Chemical Structure

Molecular Weight(MW): 199.25

APR-246, also known as 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.

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Biological Activity

Description APR-246, also known as 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.
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 MXjD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MkS5bIlocCC|ZX7zbZRqfmm2eTDhcoQh[2WubDDk[YF1cCCrbnT1Z5Rqd25iaX6gZYxtKFSSNUPteZQhdGW3a3XtbYF{NCCkdYSgcI94KEGSUj2yOFYhe2Wwc3n0bZZqfHliaX6gWHA2O3e2IFHMUC=> NELZbm0{OTB5M{C3Oi=>
UoCB-6 NH3seG9E\WyuII\pZYJqdGm2eTDhd5NigQ>? MkfMbIlocCC|ZX7zbZRqfmm2eTDhcoQh[2WubDDk[YF1cCCrbnT1Z5Rqd25iaX6gZYxtKFSSNUPteZQhdGW3a3XtbYF{NCCkdYSgcI94KEGSUj2yOFYhe2Wwc3n0bZZqfHliaX6gWHA2O3e2IFHMUC=> MoDqN|ExPzNyN{[=
EU-3 Ml;0R4VtdCC4aXHibYxqfHliYYPzZZk> NX7sWHZRcGmpaDDz[Y5{cXSrdnn0fUBidmRiY3XscEBl\WG2aDDpcoR2[3Srb36gbY4h[WyuIGTQOVNufXRibHX1b4VucWG|LDDieZQhdG:5IFHQVk0zPDZic3Xud4l1cX[rdImgbY4hXFB3M4f0JGFNVA>? NVTz[ZJpOzFyN{OwO|Y>
MUTZ-5 NWfJUZU{S2WubDD2bYFjcWyrdImgZZN{[Xl? M1rJNYhq\2hic3Xud4l1cX[rdImgZY5lKGOnbHyg[IVifGhiaX7keYN1cW:wIHnuJIFtdCCWUEWzcZV1KGyndXvlcYlieyxiYoX0JIxwfyCDUGKtNlQ3KHOnboPpeIl3cXS7IHnuJHRRPTO5dDDBUGw> NVmxZYNkOzFyN{OwO|Y>
KOPN-8 NGjGTINE\WyuII\pZYJqdGm2eTDhd5NigQ>? NH3QWVRpcWeqIIPlcpNqfGm4aYT5JIFv\CClZXzsJIRm[XSqIHnu[JVkfGmxbjDpckBidGxiVGC1N412fCCuZYXr[Y1q[XNuIHL1eEBtd3diQWDSMVI1PiC|ZX7zbZRqfmm2eTDpckBVWDV|d4SgRWxN NXL0O4NbOzFyN{OwO|Y>
RS4;11 MoDLR4VtdCC4aXHibYxqfHliYYPzZZk> M1nzSIhq\2hic3Xud4l1cX[rdImgZY5lKGOnbHyg[IVifGhiaX7keYN1cW:wIHnuJIFtdCCWUEWzcZV1KGyndXvlcYlieyxiYoX0JIxwfyCDUGKtNlQ3KHOnboPpeIl3cXS7IHnuJHRRPTO5dDDBUGw> NUTjUGpYOzFyN{OwO|Y>
SKBR3 NVHsfVdIS2WubDDjfYNt\SCjc4PhfS=> M{\ncFUhyrWP NIjTdmYzKHenZXvz MXnsZZBifGmwaXKgbY4h[2:vYnnuZZRqd25id3n0bEBCWFJvMkS2JINifXOnZDDhJIxwf2W{IHzleoVtKG:oIFexJIFzemW|dDDhcoQh[W5iaX7jdoVie2ViaX6geIhmKHO3Yj3HNUBnemGldHnvci=> M1\iXVMxPzR|OUm2
BT549 MoW2R4VtdCC4aXHibYxqfHliYYPzZZk> MoGxTWM2OD1|LkGg{txO NHTYdIw{ODF7NkKzOi=>
MDA-MB-468 NHruSVZE\WyuII\pZYJqdGm2eTDhd5NigQ>? MnHWTWM2OD13IN88US=> M1LLclMxOTl4MkO2
MDA-MB-231 Mn;hR4VtdCC4aXHibYxqfHliYYPzZZk> MVrJR|UxRTRwMTFOwG0> MnH5N|AyQTZ{M{[=
HCC1143 NHjo[3lE\WyuII\pZYJqdGm2eTDhd5NigQ>? MXHJR|UxRTZwODFOwG0> M3\TTVMxOTl4MkO2
MDA-MB-453 NEfEWIFE\WyuII\pZYJqdGm2eTDhd5NigQ>? NWfwcG4zUUN3ME2wMlkh|ryP MmTvN|AyQTZ{M{[=
SKBR3 M1juNWNmdGxidnnhZoltcXS7IHHzd4F6 MXzJR|UxRTVwMTFOwG0> NUPXUmJ3OzBzOU[yN|Y>
UACC812 M175UWNmdGxidnnhZoltcXS7IHHzd4F6 MVrJR|UxRTFzLkOg{txO NIDPOnc{ODF7NkKzOi=>
MCF7 M1PIdWNmdGxidnnhZoltcXS7IHHzd4F6 M1y0d2lEPTB;M{GuNUDPxE1? M2DLR|MxOTl4MkO2
MCF10A MUfD[YxtKH[rYXLpcIl1gSCjc4PhfS=> Mn3GTWM2OD13LkKg{txO MoqxN|AyQTZ{M{[=
UMSCC10A NH32ZoNE\WyuII\pZYJqdGm2eTDhd5NigQ>? M{jsW|AuPTBizszN NF\hSmw4OiCq M3LIepN2eHC{ZYPz[YQh[2WubDDzeZJ3cX[jbDDhcoQh[m:{ZTDhJI1w\GW|dDDl[oZm[3Rib36geIhmKGurbHzpcochd2ZiSF7TR2Mh[2WubIO= NVjCNoZZOjl|NEi0OlI>
FaDu NE\ZVY1E\WyuII\pZYJqdGm2eTDhd5NigQ>? NH[0eHcxNTVyIN88US=> MmT6O|IhcA>? NUDxWYl3e3WycILld5Nm\CClZXzsJJN2en[rdnHsJIFv\CCkb4LlJIEhdW:mZYP0JIVn\mWldDDvckB1cGVia3nscIlv\yCxZjDIUnNESyClZXzsdy=> MVSyPVM1QDR4Mh?=

... Click to View More Cell Line Experimental Data

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

Cell Research:

[1]

+ Expand
  • 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:

[1]

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

Solubility (25°C)

Chemical Information

Molecular Weight 199.25
Formula

C10H17NO3

CAS No. 5291-32-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03745716 Recruiting Drug: APR-246 + azacitidine|Drug: Azacitidine MDS Aprea Therapeutics AB January 11 2019 Phase 3
NCT03391050 Terminated Drug: APR-246|Drug: Dabrafenib Melanoma Aprea Therapeutics AB|Jules Bordet Institute January 18 2018 Phase 1|Phase 2
NCT02999893 Suspended Drug: APR-246 Oesophageal Carcinoma Peter MacCallum Cancer Centre Australia April 11 2017 Phase 1|Phase 2
NCT00900614 Completed Drug: APR-246 Hematologic Neoplasms|Prostatic Neoplasms Aprea Therapeutics AB May 2009 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID