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MCB-613

Cat. No. M5251
MCB-613 Structure
Synonym:

MCB613

Size Price Availability Quantity
10mM*1mL in DMSO USD 130  USD130 In stock
5mg USD 127  USD127 In stock
10mg USD 225  USD225 In stock
25mg USD 375  USD375 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
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.
Concentrations ~7 μM
Incubation time 48 h
Animal Experiment
Animal models Mice bearing MCF-7 xenografts
Formulation Saline
Dosages 20 mg/kg
Administration i.p.
Chemical Information
Molecular Weight 304.39
Formula C20H20N2O
CAS Number 1162656-22-5
Solubility (25°C) DMSO 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Lonard DM, et al. Clin Cancer Res. Molecular Pathways: Targeting Steroid Receptor Coactivators in Cancer.

[2] Wang L, et al. Cancer Cell. Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death.

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Keywords: MCB-613, MCB613 supplier, ROS, inhibitors, activators


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