11-Ketodihydrotestosterone (C09-1141-580)

11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a K i of 20.4 nM and an EC 50 of 1.35 nM for human AR . 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cellsIn Vitro11-Ketodihydrotestosterone (11-KDHT; 1-10 nM; 24 hours; LNCaP and VCaP cells) treatment induces significant cell proliferation. 11-Ketodihydrotestosterone (11-KDHT; 0.1-10 nM; 7-10 days; LNCaP and VCaP cells) treatment results in the significant upregulation of KLK3 , TMPRSS2 and FKBP5 in both LNCaP and VCaP cells, with the exception of KLK3 at 1 nM in LNCaP cells. In PNT2 cells, only 20% of 11β-hydroxyandrostenedione (11OHA4) and 11β-hydroxytestosterone (11OHT) are metabolised with the former yielding 11keto-androstenedione (11KA4), 11-Ketodihydrotestosterone (11-KDHT) and 11β-hydroxy-5α-androstanedione (11OH-5αDIONE) and the latter yielding 11OHA4, 11KT and 11-Ketodihydrotestosterone with downstream products <0.03 μM. In prostate cancer tissue, C11-oxy C19 metabolites at significantly higher levels than the C19 steroids are detected, with unconjugated 11-Ketodihydrotestosterone, 11KT and 11OHA4 levels ranging between 13 and 37.5 ng/g. Analyses of total steroid levels in plasma show significant levels of 11OHA4 (≈230-440 nM), 11KT (≈250-390 nM) and 11-Ketodihydrotestosterone (≈19 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: LNCaP and VCaP cells Concentration: 0.1 nM, 1 nM or 10 nM Incubation Time: 7 days (LNCaP cells) or 10 days (VCaP cells) Result: Induced significant cell proliferation. RT-PCRCell Line: LNCaP and VCaP cells Concentration: 1 nM, 10 nM Incubation Time: 24 hours Result: Resulted in the significant upregulation of KLK3 , TMPRSS2 and FKBP5 in both LNCaP (Fig 3) and VCaP (Fig 4) cells.Form:SolidIC50& Target:Ki: 20.4 nM (Human androgen receptor), EC50: 1.35 nM (Human androgen receptor). Specification: ≥98.0% Molecular Formula: C19H28O3 Molecular Weight: 304.42 PubChem CID: 11197479 Isomeric SMILES: C[C@]12CCC(=O)C[C@@H]1CC[C@@H]3[C@@H]2C(=O)C[C@]4([C@H]3CC[C@@H]4O)C