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MJC13

Cat. No. M8301
MJC13 Structure
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Biological Activity

MJC13 inhibits the positive regulation of androgen receptor (AR) signaling by the cochaperone protein FKBP52. The molecule inhibits hormone-induced dissociation of the FKBP52, nuclear translocation of AR and AR dependent gene expression. MJC13 inhibits proliferation of the androgen-dependent prostate cancer cell lines LNCaP and LAPC4.

Chemical Information
Molecular Weight 272.17
Formula C13H15Cl2NO
CAS Number 200709-97-3
Solubility (25°C) DMSO: ≥10 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] Keisuke Maeda, et al. FKBP51 and FKBP52 regulate androgen receptor dimerization and proliferation in prostate cancer cells

[2] Ji Ho Suh, et al. Similarities and Distinctions in Actions of Surface-Directed and Classic Androgen Receptor Antagonists

[3] Cheryl Storer Samaniego, et al. The FKBP52 Cochaperone Acts in Synergy with β-Catenin to Potentiate Androgen Receptor Signaling

[4] Su Liang, et al. Quantification of a New Anti-Cancer Molecule MJC13 Using a Rapid, Sensitive, and Reliable Liquid Chromatography-Tandem Mass Spectrometry Method

[5] Su Liang, et al. Solution formulation development and efficacy of MJC13 in a preclinical model of castration-resistant prostate cancer

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