1. Vitamin D Related/Nuclear Receptor Apoptosis
  2. Orphan Nuclear Receptor Androgen Receptor c-Myc
  3. XY25028

XY25028 is an orally active LRH-1 inhibitor with an IC50 of 0.30 μM. XY25028 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells and suppresses the expression of AR target genes KLK2 and KLK3. XY25028 can be used in the research of castration-resistant prostate cancer.

For research use only. We do not sell to patients.

XY25028

XY25028 Chemical Structure

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Description

XY25028 is an orally active LRH-1 inhibitor with an IC50 of 0.30 μM. XY25028 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells and suppresses the expression of AR target genes KLK2 and KLK3. XY25028 can be used in the research of castration-resistant prostate cancer[1].

In Vitro

XY25028 (96 h) inhibits the viability of 22Rv1, C4-2B and LNCaP human prostate cancer cell lines, with IC50 values of 14.46 μM, 17.41 μM and 20.88 μM, respectively[1].
XY25028 (10-40 μM; 48 h) inhibits the mRNA expression of KLK2 and KLK3 in 22Rv1 human prostate cancer cells in a dose-dependent manner[1].
XY25028 (2.5-40 μM; 48 h) inhibits c-Myc protein expression in human prostate cancer cell line 22Rv1 after 48 h of treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[1]

Cell Line: 22Rv1 human prostate cancer cells
Concentration: 10 μM, 20 μM, 40 μM
Incubation Time: 48 h
Result: Significantly reduced KLK3 mRNA levels.

Western Blot Analysis[1]

Cell Line: 22Rv1 human prostate cancer cells
Concentration: 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 48 h
Result: Significantly reduced c-Myc protein expression at 20 μM and 40 μM compared to vehicle control.
Showed no significant changes in c-Myc protein expression at 2.5 μM, 5 μM, or 10 μM compared to vehicle control.
In Vivo

XY25028 (50 mg/kg; p.o.; once daily; 16 days) elicits significant antitumor efficacy in a 22Rv1 CRPC xenograft model, with a 40.7% tumor growth inhibition rate and no detectable systemic toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c-Nude (male, 5 weeks old)[1]
Dosage: 50 mg/kg
Administration: p.o.; once daily; 16 consecutive days
Result: Achieved a tumor growth inhibition (TGI) rate of 40.7%.
Showed no significant body weight changes (a marker of systemic toxicity) throughout the 16-day study period.
Molecular Weight

498.66

Formula

C32H38N2O3

SMILES

NC1=CC=C(N(CC2=CC=CC=C2)C=C3C4=CC=C(OCCCCCCC(OC(C)(C)C)=O)C=C4)C3=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
XY25028
Cat. No.:
HY-181971
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