|Description||AMG232 is an extremely potent MDM2 inhibitor with remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft model (ED50 = 9.1 mg/kg). AMG232 is currently under clinical development.|
|Synonyms||AMG-232; AMG 232.|
Nutlin-3a is an inhibitor of MDM2 (human homolog of murine double minute 2), which disrupts its interaction with p53, leading to the stabilization and activatio...
Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.
AMG232 is an extremely potent MDM2 inhibitor with remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft mode...
RO8994, a spiroindolinone derivative, is an effective MDM2 inhibitor and has been found to have prabable activity against haematological malignancies. IC50: 5 n...
Nutlin-3 is MDM2 antagonist, inhibits p53-Mdm2 interaction (IC50=0.09 µM).
NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibit...
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
RITA (NSC 652287)
RITA is an inhibitor of p53-HDM-2 interaction, which binds to p53dN with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.