Galeterone CAS: 851983-85-2
MF: C26H32N2O
MW: 388.55
Galeterone is an antagonist to LNCaP AR.

Galeterone (CAS 851983-85-2)

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Alternate Names: TOK-001
Application: Galeterone is an antagonist to LNCaP AR
CAS Number: 851983-85-2
Purity: ≥98%
Molecular Weight: 388.55
Molecular Formula: C26H32N2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Galeterone is effective at preventing binding of [3H]-R1881 to the mutant LNCaP AR (T877A) and to T575A mutant AR in PC3 cells with IC50 values of 845 nM and 454 nM, respectively. The effects on AR significantly reduce cellular phospho-4EBP1 levels. Galeterone potently inhibits the proliferation of LNCaP and LAPC4 cells in the with IC50 values of 2.6 μM and 4 μM, respectively. Galeterone induces the endoplasmic reticulum s.tress response resulting in down-regulation of cyclin D1 protein expression and cyclin E2 mRNA in vitro. Galeterone is a selective CYP17 inhibitor and AR (androgen receptor) antagonist


References

1. Handratta VD, et al. J Med Chem, 2005, 48(8), 2972-2984. 2. Vasaitis T, et al. Mol Cancer Ther, 2008, 7(8), 2348-2357. 3. Bruno RD, et al. Mol Cancer Ther, 2008, 7(9), 2828-2836. 4. Schayowitz A, et al. Mol Cancer Ther, 2008, 7(1), 121-132. 5. Schayowi

Physical State :
Solid
Storage :
Store at -20° C
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
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Certificate of Analysis

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PMID: # 27174722  Bogner, J. et al. 2017. J. Steroid Biochem. Mol. Biol. 166: 45-53.

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