AM-8735 is a potent and selective MDM2 inhibitor with an IC₅₀ of 25 nM.

IC50: 25 nM (MDM2)^[1]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

568.51

C₂₇H₃₁Cl₂NO₆S

1429386-01-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.