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RO8994 induces dose-dependent up-regulation of p53 target genes and apoptosis in wild-type p53 cancer cells, consistent with its non-genotoxic mechanism of p53 activation.
In vivo, RO8994 displays remarkable tumor growth inhibition in the wild-type p53, MDM2-amplified SJSA-1 osteosarcoma tumor xenograft model - exhibiting significant (>60%) tumor growth inhibition at the low dose of 1.56 mg/kg, tumor stasis at 3.125 mg/kg and regression at 6.25 mg/kg.
| Molecular Weight | 613.51 |
| Formula | C31H31Cl2FN4O4 |
| CAS Number | 1309684-94-3 |
| Solubility (25°C) | DMSO: ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Mdm2 Products |
|---|
| Nutlin-3
Nutlin-3 is a selective MDM2 (mouse double minute 2) antagonist with IC50 of 90 nM. Nutlin-3 induces apoptosis in cancer cells. Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM in cells with wild-type p53 such as HCT116, RKO and SJSA-1. |
| NSC 66811
NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM, which disrupts MDM2-p53 interaction and activates p53 function. |
| Nutlin-3a
Nutlin-3a, the active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits the p53/MDM2 interaction with IC50 of 90 nM. |
| Nutlin-3b
Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite enantiomer Nutlin-3a. |
| SL-01
SL-01 is a p53-Mdm2 interaction inhibitor with IC50 of 3.18 μM. |
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