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PRIMA-1

Catalog No. T6954 CAS 5608-24-2

Synonyms: 2,2-Bis(hydroxymethyl)-3-quinuclidinone, NSC-281668, PRIMA 1

PRIMA-1 (NSC-281668) is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PRIMA-1, CAS 5608-24-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 67.00
25 mg	In stock	$ 143.00
50 mg	In stock	$ 217.00
100 mg	In stock	$ 387.00
200 mg	In stock	$ 576.00
500 mg	In stock	$ 923.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Description	PRIMA-1 (NSC-281668) is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.
In vitro	PRIMA-1 is converted to compounds that form adducts with thiols in mutant p53. Modification of thiol groups in mutant p53 by PRIMA-1 conversion products is sufficient to restore its tumor suppressor activity.[2]. PRIMA-1 inhibits the growth of pancreatic cancer cell lines and induces cell cycle arrest and decreases DNA synthesis. It selectively induces apoptosis and cell death in mutant p53-expressing pancreatic cancer cells and also leads to activation of p53-dependent apoptotic pathways. PRIMA-1 enhances the cytotoxicity of chemotherapeutic agents active against mutant p53 pancreatic cancer cells[1]. PRIMA-1 has antileukemic properties in acute promyelocytic leukemia-derived NB4 cells. PRIMA-1-triggered apoptosis is in a dose-dependent and time-dependent manner as indicated by the MTT assay and annexin-V staining. Apoptosis induction by PRIMA-1 is associated with caspase-9, caspase-7 activation and PARP cleavage. PRIMA-1 does not show any significant apoptotic effect in normal human peripheral blood mononuclear cells[4].
In vivo	Intravenous (i.v.) injections of PRIMA-1 in mice does not cause any obvious changes in weight or behavior compared with untreated animals. PRIMA-1 has in vivo antitumor activity in this animal tumor model. It suppresses in vivo tumor growth in a mutant p53-dependent manner[3].
Cell Research	Cells are kept at a temperature of 37 °C, a minimum relative humidity of 95 %, and an atmosphere of 5 % CO2 in air. Cell viability is measured by MTT assay after treatment with PRIMA-1. Briefly, cells are seeded in each well of 96-well plates in 100 μl culture medium and incubated overnight at 37 °C in an atmosphere of 5 % CO2. The next day, the medium is removed and cells washed with PBS and treated with vehicle control(DMSO, dimethylsulfoxide) or different concentrations of PRIMA-1 for 12 to 48 h; the medium is replaced with MTT solution diluted in medium once the treatment is completed. The plates are further incubated at 37 °C under 5 % CO2 for 4 h and then left at room temperature until completely dry. DMSO was then added and the absorbance is read at 492 nm using a microplate enzyme-linked immunoassay reader (ELISA). The relative growth activity is determined as the percentage absorbance of treated cells compared to that of vehicle treated cells (control).(Only for Reference)

Synonyms	2,2-Bis(hydroxymethyl)-3-quinuclidinone, NSC-281668, PRIMA 1
Molecular Weight	185.22
Formula	C9H15NO3
CAS No.	5608-24-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 35 mg/mL(189 mM)

H2O: 18.5 mg/mL(100 mM)

DMSO: 50 mg/mL (269.95 mM)

References and Literature

1. Izetti P, et al. Invest New Drugs. 2014, 32(5):783-94. 2. Lambert JM, et al. Cancer Cell. 2009, 15(5):376-88. 3. Bykov VJ, et al. Nat Med. 2002, 8(3):282-8. 4. Farhadi E, et al. Anticancer Drugs. 2016.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Cell Cycle Compound Library Anti-Pancreatic Cancer Compound Library Anti-Aging Compound Library NO PAINS Compound Library Pyroptosis Compound Library Anti-Cancer Metabolism Compound Library Preclinical Compound Library Anti-Lung Cancer Compound Library

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Keywords

PRIMA-1 5608-24-2 Apoptosis Autophagy Others Ferroptosis NSC 281668 PRIMA1 2,2-Bis(hydroxymethyl)-3-quinuclidinone NSC-281668 inhibit MDM-2/p53 NSC281668 Inhibitor PRIMA 1 inhibitor

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