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.

Size Price Stock Quantity  
USD 97 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective p53 Inhibitors

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.
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{[=
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].


Cell Research:


+ 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:


+ 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


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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

p53 Signaling Pathway Map

Related p53 Products

Tags: buy APR-246 (PRIMA-1MET) | APR-246 (PRIMA-1MET) supplier | purchase APR-246 (PRIMA-1MET) | APR-246 (PRIMA-1MET) cost | APR-246 (PRIMA-1MET) manufacturer | order APR-246 (PRIMA-1MET) | APR-246 (PRIMA-1MET) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID