RO8994
Modify Date: 2024-01-07 18:05:09
RO8994 structure
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Common Name | RO8994 | ||
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| CAS Number | 1309684-94-3 | Molecular Weight | 613.50700 | |
| Density | 1.41±0.1 g/cm3 (20 ºC ,760 mmHg), 计算值 | Boiling Point | N/A | |
| Molecular Formula | C31H31Cl2FN4O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of RO8994RO8994 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: MDM2in 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. |
| Name | ro8994 |
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| Synonym | More Synonyms |
| Description | 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: MDM2in 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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| Related Catalog | |
| References |
| Density | 1.41±0.1 g/cm3 (20 ºC ,760 mmHg), 计算值 |
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| Molecular Formula | C31H31Cl2FN4O4 |
| Molecular Weight | 613.50700 |
| Exact Mass | 612.17100 |
| PSA | 122.55000 |
| LogP | 6.86910 |
| Storage condition | 2-8℃ |
| (2'S,3R,4'R,5'R)-N-(4-carbamoyl-2-methoxyphenyl)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-neopentyl-2-oxospiro[indoline-3,3'-pyrrolidine]-5'-carboxamide |
| Spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide, N-[4-(aminocarbonyl)-2-methoxyphenyl]-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-2-oxo-, (2'S,3R,4'R,5'R)- |
| RO 8994 |
| RO-8994 |