product name RG-7112
References: Pediatr Blood Cancer. 2013 Apr;60(4):633-41. Exp Hematol. 2014 Feb;42(2):137-45.e5.
726.28
Formula
C38H48Cl2N4O4S
CAS No.
939981-39-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (137.7 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol:
Solubility (In vivo)
1% CMC Na:14mg/mL
Chemical Name
[(4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethylimidazol-1-yl]-[4-(3-methylsulfonylpropyl)piperazin-1-yl]methanone
other peoduct :
| RG7112 has been profiled extensively in many cell lines. In 15 cancer cell lines expressing wild-type p53, it shows IC50 in the range of 0.18 – 2.2 μM. However, the inhibition is much less in seven cancer cell lines with p53 mutation, IC50 5.7 – 20.3 μM. The overall selectivity is 14-fold. | |
|---|---|
| In Vivo | In the SJSA1 xenograft mouse model, RG7112 (200 mg/kg, p.o.) penetrates tumor cells and activate p53 and its 2 major functions, cell-cycle arrest and apoptosis. In nude mice bearing SJSA-1, and MHMn xenografts, RG7112 (100 mg/kg, p.o.) causes tumor regression. In rats, RG7112 impairs thrombopoiesis via activation of p53. |
| Animal model | SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice |
| Formulation & Dosage | 1% Klucel LF/0.1% Tween 80; 200 mg/kg; oral taken |
| References | [1]Pediatr Blood Cancer 2013;60:633–641 |
