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  3. XY25026

XY25026 is an orally active LRH-1 inhibitor with an IC50 of 0.28 μM. XY25026 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells, suppresses the expression of AR target genes KLK2 and KLK3, and inhibits tumor growth in xenograft models. XY25026 is applicable to the research of castration-resistant prostate cancer.

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

XY25026

XY25026 Chemical Structure

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Description

XY25026 is an orally active LRH-1 inhibitor with an IC50 of 0.28 μM. XY25026 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells, suppresses the expression of AR target genes KLK2 and KLK3, and inhibits tumor growth in xenograft models. XY25026 is applicable to the research of castration-resistant prostate cancer[1].

In Vitro

XY25026 (1 h) potently inhibits the interaction between human LRH-1 LBD and SRC1 coactivator peptide in a cell-free AlphaScreen assay with an IC50 of 280 nM[1].
XY25026 (96 h) inhibits proliferation of 22Rv1, C4-2B, and LNCaP human prostate cancer cell lines with IC50 values of 13.29 μM, 14.56 μM, and 15.89 μM, respectively[1].
XY25026 (0-40 μM; 48 h) suppresses expression of AR target genes KLK2 and KLK3, and the oncogenic protein c-Myc, in 22Rv1 human prostate cancer cells[1].

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

Real Time qPCR[1]

Cell Line: 22Rv1 cells
Concentration: 0, 10, 20 and 40 μM
Incubation Time: 48 h
Result: Suppressed expression of AR target genes KLK2 and KLK3.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0, 2.5, 5, 10, 20 and 40 μM
Incubation Time: 48 h
Result: Inhibited the expression of c-Myc.
Parmacokinetics
Species Dose Route Cmax Tmax AUC0-t AUC0-∞ T1/2 CL F
Rat[1] 1 mg/kg i.v. 578 ng/mL 0.083 h 343 ng·h/mL 346 ng·h/mL 1.28 h 3071 mL/h/kg /
Rat[1] 5 mg/kg p.o. 37.1 ng/mL 0.833 h 94.6 ng·h/mL 98.5 ng·h/mL 1.63 h / 5.69 %
In Vivo

XY25026 (50-100 mg/kg; p.o.; once daily; 16 days) achieves tumor growth inhibition rates of 31.5% and 44.6%, respectively, in a 22Rv1 castration-resistant prostate cancer xenograft model with 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; 100 mg/kg
Administration: p.o.; once daily; 16 days
Result: Achieved a tumor growth inhibition (TGI) rate of 31.5%.
Achieved a tumor growth inhibition (TGI) rate of 44.6%.
Showed no significant body weight changes (a marker of systemic toxicity) throughout the study.
Molecular Weight

470.60

Formula

C30H34N2O3

SMILES

NC1=CC=C(N(CC2=CC=CC=C2)C=C3C4=CC=C(OCCCCC(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
References
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Help & FAQs
  • 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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XY25026
Cat. No.:
HY-181970
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