Name | AM-8735 |
---|
Description | AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM. |
---|---|
Related Catalog | |
Target |
IC50: 25 nM (MDM2)[1] |
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]. |
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]. |
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]. |
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]. |
References |
Molecular Formula | C27H31Cl2NO6S |
---|---|
Molecular Weight | 568.51 |