AM-8735是有效,选择性的 MDM2 抑制剂,IC50 值为25 nM。
Description | AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM. | ||||||||||||||||
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IC50 & 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]. | ||||||||||||||||
Solvent & Solubility | In Vitro: 10 mM in DMSO Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References |
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