| Description |
AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM.
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| Related Catalog |
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| Target |
IC50: 25 nM (MDM2)[1]
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| In Vitro |
AM-8735 displays substantial growth inhibition of wild-type p53 cells (IC50=63 nM) and no growth inhibition of p53-deficient cells (IC50>25 μM). AM-8735exhibits a dose-dependent increase of p21 mRNA, a direct transcriptional readout of p53 activity, in HCT116 p53wt cells (IC50=160 nM)[1].
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| In Vivo |
AM-8735 also demonstrates significant time and concentration dependent p21 mRNA induction in vivo in a pharmacodynamic assay in SJSA-1 osteosarcoma tumors. AM-8735 shows excellent antitumor activity in the SJSA-1 osteosarcoma xenograft model with an ED50 of 41 mg/kg[1].
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| Cell Assay |
SJSA-1 cells cells are treated with AM-8735 for 16 hours in the presence of 10% human serum. Cell proliferation is measured by the Click-iT EdU assay[1].
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| Animal Admin |
Rats[1] SJSA-1 cells (5 × 106) are implanted subcutaneously into female athymic nude mice. AM-8735 is administered by oral gavage (as a solution in 15% HPβCD, 1% Pluronic F68, pH 8) 5, 25, 50, and 100 mg/kg q.d. for a period of 2 weeks, and tumor volume is quantified[1].
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| References |
[1]. Gonzalez AZ, et al. Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction. J Med Chem. 2014 Mar 27;57(6):2472-88.
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