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APR-246 (PRIMA-1MET)

Catalog No.: 17021316
Cas No.: 5291-32-7
Purity : 98% 
17021316 - APR-246 (PRIMA-1MET) | CAS 5291-32-7

Catalog number : 17021316

CAS number : 5291-32-7

Molecular Formula : C10H17NO3 

Molecular Weight : 199.25 

Iupac Chemical Name : APR-246 (PRIMA-1MET) 

Smile : COCC1(C(=O)[C@H]2CCN1CC2)CO

InChiKey : BGBNULCRKBVAKL-UHFFFAOYSA-N

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SynonymsN/A 
Molecular FormulaC10H17NO3 
Molecular Weight199.25 
Appearancecrystalline solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
SmileCOCC1(C(=O)[C@H]2CCN1CC2)CO
InChiKeyBGBNULCRKBVAKL-UHFFFAOYSA-N
InChiInChI=1S/C10H17NO3/c1-14-7-10(6-12)9(13)8-2-4-11(10)5-3-8/h8,12H,2-7H2,1H3
MDLMFCD16294187
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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.

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. 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.

 

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