PRIMA-1 Struktur

PRIMA-1

Bezeichnung:PRIMA-1

CAS-Nr5608-24-2

Englisch Name:PRIMA-1

CBNumberCB8165699

SummenformelC9H15NO3

Molgewicht185.22

MOL-Datei5608-24-2.mol

PRIMA-1 physikalisch-chemischer Eigenschaften

Schmelzpunkt	146-147 °C
Siedepunkt	353.7±17.0 °C(Predicted)
Dichte	1.32±0.1 g/cm3(Predicted)
storage temp.	Inert atmosphere,2-8°C
Löslichkeit	H2O: >10mg/mL
pka	13.68±0.10(Predicted)
Aggregatzustand	solid
Farbe	white to off-white
Wasserlöslichkeit	Soluble in water at 10mg/ml
Sensitive	Light Sensitive

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-43
S-Sätze:	36/37
WGK Germany	3

Gefahreninformationscode (GHS)

PRIMA-1 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
PRIMA-1 is a reactivator of p53 and inducer of apoptosis.
Definition
ChEBI: 2,2-bis(hydroxymethyl)-1-azabicyclo[2.2.2]octan-3-one is a member of quinuclidines and a cyclic ketone.
Biologische Aktivität
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.
Lager
Store at +4°C
Einzelnachweise
[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.

PRIMA-1 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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