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MCB-613

Cat. No. M5251
MCB-613 Structure
Size Price Availability Quantity
10mM/1mL In DMSO USD 130 In stock
5mg USD 127 In stock
10mg USD 210 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 304.39
Formula C20H20N2O
CAS Number 1162656-22-5
Purity >98%
Solubility 60 mg/mL warmed in DMSO
Storage at -20°C
References

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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  Catalog
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Keywords: MCB-613 supplier, Src-bcr-Abl, inhibitors

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