Network Version
RO8994 Data Sheet
| Product Name: | RO8994 |
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|---|---|---|
| CAS No.: | 1309684-94-3 | |
| Cat. No.: | HY-16999 | |
| MWt: | 613.51 | |
| Formula: | C31H31Cl2FN4O4 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 45 mg/mL (73.35 mM) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| RO8994 is a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitor, with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). IC50 value: 5 nM (in HTRF binding assays), 20 nM (in MTT proliferation assays) Target: MDM2 in vitro: RO8994 represents a new generation of p53-MDM2 antagonists with marked improvement in pharmacological properties for potential clinical development. 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. | ||
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