5608-24-2 Usage
Uses
PRIMA-1 is a reactivator of p53 and inducer of apoptosis.
Biological Activity
Selectively restores mutant p53 activity in tumor cells via activation of Bax and PUMA. Induces apoptosis and inhibits growth of human tumors with mutant p53.
in vitro
the substantial increase in saos-2-his-273-cells death could be noticed after being treated with 125 μm prima-1 for 48 hours. tunel staining revealed that such tumor-cell death was primarily triggered by apoptosis. prima-1 could also restore the transcriptional transactivation function to mutant p53 in vitro. [2]
in vivo
to assess the effect of prima-1 on human tumor xenografts, mice were inoculated with saos-2-his-273 cells expressing mutant p53. the mice then received prima-1 treatment at intra-tumor does of 20 mg/kg or i.v. doses of 20 and 100 mg/kg twice a day for three days. compared with the control group, the average tumor volume decreased from 555.7 mm3 to 11.7 (100 mg/kg) and 53 (20 mg/kg) mm3 after i.v. injections of prima-1. intra-tumor injections of prima-1 also decreased the average tumor volume to 5.3 mm3. [2]
IC 50
the value varied among different tumor type. in saos-2-his-273 cells, prima-1 induced cell death with an ic50 of over 15 m.
references
[1] bykov v, issaeva n, zache n, shilov a, hultcrantz m, bergman j, selivanova g, wiman kg. reactivation of mutant p53 and induction of apoptosis in human tumor cells by maleimide analogs. j biol chem. 2005 aug; 280(34): 30384–91. [2] bykov v, issaeva n, shilov a, hultcrantz m, pugacheva e, chumakov p, bergman j, wiman kg, selivanova g. restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound. nat med. 2002 mar; 8(3):282-8. [3] lehmann s, bykov v, ali d, andren o, cherif h, tidefelt u, uggla b, yachnin j, juliusson g, moshfegh a, paul c, wiman kg, andersson po. targeting p53 in vivo: a first-in-human study with p53-targeting compound apr-246 in refractory hematologic malignancies and prostate cancer. j clin oncol. 2012. doi: 10.1200/jco.2011.40.7783.
Check Digit Verification of cas no
The CAS Registry Mumber 5608-24-2 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 5,6,0 and 8 respectively; the second part has 2 digits, 2 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 5608-24:
(6*5)+(5*6)+(4*0)+(3*8)+(2*2)+(1*4)=92
92 % 10 = 2
So 5608-24-2 is a valid CAS Registry Number.
InChI:InChI=1/C9H15NO3/c11-5-9(6-12)8(13)7-1-3-10(9)4-2-7/h7,11-12H,1-6H2
5608-24-2Relevant articles and documents
QUINUCLIDINONE DERIVATIVES AS ANTICANCER AGENTS
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Page/Page column 7, (2008/06/13)
New compounds of formula (I): wherein R1 and R2 may be the same or different and are selected from H, halo, alkyl, cycloalkyl, haloalkyl, aryl, haloaryl, alkylaryl, alkoxyaryl, hydroxyl, acetate, ketal, alkoxy, and combinations there
AZABICYCLOOCTAN-3-ONE DERIVATIVES AND USE THEREOF
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Page/Page column 12-13, (2010/02/14)
Compounds of Formula (I) processes for preparing them, pharmaceutical compositions comprising them. The use of compounds of formula (I) for hyperproliferative diseases, e.g. cancer as well as autoimmune diseases and heart diseases.
OPTICAL IMAGING CONTRAST AGENTS FOR IMAGING LUNG CANCER
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Page/Page column 21, (2008/06/13)
The invention provides contrast agents for optical imaging of lung cancer in patients. The contrast agents may be used in diagnosis of lung cancer, for follow up of progress in disease development, for follow up of treatment of lung cancer and for surgica
