RO8994 |
| Catalog No.GC19312 |
RO8994 est une série très puissante et sélective d'inhibiteurs MDM2 À petite molécule de spiroindolinone, avec une IC50 de 5 nM (tests de liaison HTRF) et 20 nM (tests de prolifération MTT).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1309684-94-3
Sample solution is provided at 25 µL, 10mM.
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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.
References:
[1]. Zhang Z, et al. Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg Med Chem. 2014 Aug 1;22(15):4001-4009.
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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