product name Nutlin-3a
References: Science. 2004 Feb 6;303(5659):844-8; Clin Cancer Res. 2009 Feb 1;15(3):933-42.
581.49
Formula
C30H30Cl2N4O4
CAS No.
675576-98-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (171.97 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol:
Solubility (In vivo)
5% DMSO+55% PEG 300+ddH2O: 8 mg/mL
Chemical Name
4-[(4S,5R)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
other peoduct :
| Nutlin-3a stabilizes and activates p53, and induces p21 expression in a dose-dependent manner. Nutlin-3a effectively depletes the S-phase compartment to 0.2-2% and increases the G1- and G2/M-phase compartments. Nutlin-3a induces apoptosis in ~60% of SJSA-1 and MHM cells after 40 h, which increased further after 60 h (85% and 65%, respectively) | |
|---|---|
| In Vivo | Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage. Nutlin-3 is a selective activator of the p53 pathway in vivo and highly efficacious against SJSA-1 osteosarcoma tumors |
| Animal model | Nude mice bearing subcutaneous human cancer xenografts |
| Formulation & Dosage | 1% Klucel, 0.1% Tween 80; 100, 200 mg/kg; p.o.; b.i.d |
| References | [1] Tovar C, et al. Proc Natl Acad Sci U S A, 2006, 103(6), 1888-1893. |
