PRIMA-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种特定突变型 p53 重激活剂，可诱导癌细胞系凋亡并增强化疗细胞毒性。

A specific mutant p53 reactivator that induces apoptosis and enhances chemotherapeutic cytotoxicity in cancer cell lines; is efficacious against myeloma cells with differential p53 genotypes, causes the demethylation of TP73, through DNMT1 depletion, to subsequently enhance UPR; selectively induces apoptosis and cell cycle arrest in p53 mutant cells compared to CAPAN-2 cells.Blood Cancer Phase 2 Clinical.

The cell lines are cultured in the presence of PRIMA-1 (NSC-281668) at 0-140 μM. The IC50s are 35, 40, 50, 50, 60, 70 and 75 μM for PANC-1, HEC-1-B, SUM149, AN 3CA, Ishikawa, Panc02 and MDA-MB-231 cells, respectively.

PRIMA-1 (Prima-1) is a p53-modulating agent. 150 or 300 ppm PRIMA-1 significantly suppresses (P<0.0001) lung adenocarcinoma formation by 56% and 62%, respectively, after 17 weeks and 39% and 56%, respectively, after 34 weeks. Administration of 150 or 300 ppm PRIMA-1 significantly suppresses NNK-induced total lung adenocarcinoma formation by 57% or 62% (P<0.0001), respectively, after 17 weeks of exposure and by 39% or 56% (P<0.0001), respectively, after 34 weeks of exposure. As with administration of the lower (50 ppm) dose of CP-31398, administration of the lower (150 ppm) dose of PRIMA-1also slightly increases the number of NNK-induced lung adenomas.

PRIMA 1 | PRIMA1

Apoptosis

MDM2-p53

p53

Cancer

Blood cancer

5608-24-2

185.2203

C9H15NO3

>98% (HPLC)

DMSO: ≥ 44 mg/mL

O=C1C(CO)(CO)N2CCC1CC2

1-Azabicyclo[2.2.2]octan-3-one, 2,2-bis(hydroxymethyl)-

(-20℃)

With Ice Pack

≥ 2 years