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NSC 66811

Cat. No. M2207
NSC 66811 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 100 In stock
50mg USD 260 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 340.42
Formula C23H20N2O
CAS Number 6964-62-1
Purity 100.00%
Solubility DMSO 20 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Acta Pharmacol Sin (2015). Figure 2. NSC 66811
Method PCR
Cell Lines HepG2 cells
Concentrations 5 and 25 μmol/L
Incubation Time 24 h
Results The p53 mRNA levels were up-regulated by NSC 66811 (Figure 2F) without affecting the CYP expression. NSC 66811 decreased the metabolism of DEM (Figure 2G) and TEST (Figure 2H) in a dose-dependent manner.
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References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: NSC 66811 supplier, Mdm2, inhibitors

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