NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM, which disrupts MDM2-p53 interaction and activates p53 function. NSC-66811 induces p21, p53 and MDM2 accumulation in human colon cancer cells in vitro. NSC 66811 is more potent than the natural p53 peptide to bind with MDM2.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL|
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy.
Shangary S, et al. Annu Rev Pharmacol Toxicol. 2009;49:223-41. PMID: 18834305.
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.
Lu Y, et al. J Med Chem. 2006 Jun 29;49(13):3759-62. PMID: 16789731.
|Related Mdm2 Products|
MI-773 is an orally available MDM2 antagonist with Ki of 0.88 nM.
Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2.
NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.
SL-01 is a p53-Mdm2 interaction inhibitor with IC50 of 3.18 μM.
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