In vitro: MCB-613 selectively and reversibly binds to the RID of SRC-3, and selectively kills cancer cells including MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells, without toxicity to mouse primary hepatocytes and mouse embryonic fibroblasts (MEFs). MCB-613 also increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS).
In vivo: In an MCF-7 breast cancer mouse xenograft model, MCB-613 (20 mg/kg, i.p.) significantly and dramatically inhibits the growth of the tumor while causing no obvious animal toxicity and body weight less.
|Cell lines||MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells; mouse primary hepatocytes and mouse embryonic fibroblasts|
|Preparation method||Cells are seeded in 96-well plates and allowed to reach 60% to 70% confluence. After indicated compound treatments, relative numbers of viable cells are measured by MTS assay using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay.|
|Incubation time||48 h|
|Animal models||Mice bearing MCF-7 xenografts|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||60 mg/mL warmed in DMSO|
Molecular Pathways: Targeting Steroid Receptor Coactivators in Cancer.
Lonard DM, et al. Clin Cancer Res. 2016 Nov 15;22(22):5403-5407. PMID: 27654711.
Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death.
Wang L, et al. Cancer Cell. 2015 Aug 10;28(2):240-52. PMID: 26267537.
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