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RO8994

CAS No. : 1309684-94-3

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.

Research Area：Cancer

Targets：MDM-2/p53|Apoptosis|E1/E2/E3 Enzyme

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Related Small Molecules:Physalin A;Bomedemstat ditosylate;Enpp/Carbonic anhydrase-IN-1;GK563;Calpeptin;Lobetyolin;UBE2T/FANCL-IN-1;BJE6-106;Dinaciclib;Ecteinascidin 770;MDM2-p53-IN-15;AT9283;Staurosporine;SNS-032;C188-9;ZLDI-8;Topoisomerase I/II inhibitor 3;Xevinapant;Mangiferin;Cambinol;Antioxidant agent-5;Apoptosis inducer 9;Bafetinib;Cyclovirobuxine D

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