Product Name
APR-246 (PRIMA-1MET)
Iupac Chemical Name
APR-246 (PRIMA-1MET)
Synonyms
N/A
Molecular Formula
C10H17NO3
Molecular Weight
199.25
Smile
COCC1(C(=O)[C@H]2CCN1CC2)CO
InChiKey
BGBNULCRKBVAKL-UHFFFAOYSA-N
InChi
InChI=1S/C10H17NO3/c1-14-7-10(6-12)9(13)8-2-4-11(10)5-3-8/h8,12H,2-7H2,1H3
Cas
5291-32-7
MDL
MFCD16294187
Appearance
crystalline solid
Purity
98%
Solubility
Soluble in DMSO
Storage
3 years -20ºCpowder
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical.
Quality control
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.
Advantages:
Hubei XinRunde Chemical Co., Ltd is a renowned pharmaceutical manufacturer. We can offer high quality products at competitive price in quick delivery with 100% custom pass guaranteed. Never stop striving to offer our best service is our philosophy. We have Flexible and Untraceable payment terms. As a leading manufacture, our products have been exported to Germany, Norway, Poland, Finland, Spain, UK, France, Russia, USA, Brazil, Mexico, Australia, Japan, Korea, Thailand, Indonesia, Uruguay and many other countries.
1. Quality.Every batch of steroid powders have tobetested by our QC(quality control) before they are allowed to sell.
2 . Delivery We have stock, so we can delivery quickly at the very day when receive the payment. Within 24 hours after receiving the payment Lead time 4 or 7 days.
3 . Discreet package Safelyand Professionally Disguised Package Guaranteed. For your safety and to insure delivery all products will be packed in a discreet way to prevent any suspicions, no steroids related name will appear on the parcels. high successful delivery rate
4 . Warm after-sale service Any of your question would be solved for the first as soon as possible.