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Ralaniten

Cat. No. M10960
Ralaniten Structure
Synonym:

EPI-002

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Biological Activity

Ralaniten (EPI-002) is an effective and orally active androgen receptor N-terminal domain (AR-NTD) antagonist. Ralaniten inhibits AR transcriptional activity,IC50 The value is 7.4 μM. Ralanites can be used in the study of castration-resistant prostate cancer (CRPC).

Chemical Information
Molecular Weight 394.89
Formula C21H27ClO5
CAS Number 1203490-23-6
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage 4°C, protect from light, dry, sealed
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] Jacky K Leung, et al. Commun Biol. Pin1 inhibition improves the efficacy of ralaniten compounds that bind to the N-terminal domain of androgen receptor

[2] Carmen A Banuelos, et al. Cancers (Basel). Ralaniten Sensitizes Enzalutamide-Resistant Prostate Cancer to Ionizing Radiation in Prostate Cancer Cells that Express Androgen Receptor Splice Variants

[3] Jon K Obst, et al. ACS Pharmacol Transl Sci. Revealing Metabolic Liabilities of Ralaniten To Enhance Novel Androgen Receptor Targeted Therapies

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Keywords: Ralaniten, EPI-002 supplier, Androgen Receptor, inhibitors, activators


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