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RO8994 Chemical Structure
|Product name: RO8994|
|Cat. No.: HY-16999|
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)
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.
|M.Wt||613.51||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
|1 mg||5 mg||10 mg|
|1 mM||1.6300 mL||8.1498 mL||16.2997 mL|
|5 mM||0.3260 mL||1.6300 mL||3.2599 mL|
|10 mM||0.1630 mL||0.8150 mL||1.6300 mL|
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