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1203490-23-6

1203490-23-6 Structure

1203490-23-6 Structure
IdentificationBack Directory
[Name]

(R)-3-(4-(2-(4-((S)-3-chloro-2-hydroxypropoxy)phenyl)propan-2-yl)phenoxy)propane-1,2-diol
[CAS]

1203490-23-6
[Synonyms]

EPI002
(R)-3-(4-(2-(4-((S)-3-chloro-2-hydroxypropoxy)phenyl)propan-2-yl)phenoxy)propane-1,2-diol
1,2-Propanediol, 3-[4-[1-[4-[(2S)-3-chloro-2-hydroxypropoxy]phenyl]-1-methylethyl]phenoxy]-, (2R)-
[Molecular Formula]

C21H27ClO5
[MDL Number]

MFCD30502912
[MOL File]

1203490-23-6.mol
[Molecular Weight]

394.89
Chemical PropertiesBack Directory
[Boiling point ]

601.0±55.0 °C(Predicted)
[density ]

1.228±0.06 g/cm3(Predicted)
[storage temp. ]

4°C, protect from light
[solubility ]

DMSO : 100 mg/mL (253.24 mM; Need ultrasonic)
[form ]

Solid
[pka]

13.13±0.20(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC)[1][2].
[in vivo]

EPI-002 (100 mg/kg; p.o. twice daily for 28 days) inhibits the VCaP tumor growth in castrated mice[1].

Animal Model:Male NOD-SCID mice bearing subcutaneous tumors were castrated
Dosage:100 mg/kg
Administration:P.o. twice daily for 28 days
Result:Inhibited the growth of castration-resistant prostate cancer (CRPC) xenografts that express AR splice variants[1].
[storage]

4°C, protect from light
[References]

[1] Myung JK, et, al. An androgen receptor N-terminal domain antagonist for treating prostate cancer. J Clin Invest. 2013 Jul;123(7):2948-60. DOI:10.1172/JCI66398
[2] Yang YC, et, al. Targeting Androgen Receptor Activation Function-1 with EPI to Overcome Resistance Mechanisms in Castration-Resistant Prostate Cancer. Clin Cancer Res. 2016 Sep 1;22(17):4466-77. DOI:10.1158/1078-0432.CCR-15-2901
Spectrum DetailBack Directory
[Spectrum Detail]

(R)-3-(4-(2-(4-((S)-3-chloro-2-hydroxypropoxy)phenyl)propan-2-yl)phenoxy)propane-1,2-diol(1203490-23-6)1HNMR
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