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Cat. No.: HY-181970

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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.

Formula: C₃₀H₃₄N₂O₃
Molecular Weight:470.60

Storage:

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

XY25026 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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	C_max	T_max	AUC_0-t	AUC_0-∞	T_1/2	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.

Chemical Information

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

Handling Instructions (2659 KB)

References

[1]. Ma K, et al. Discovery of novel indole derivatives as LRH-1 antagonists for the treatment of castration resistant prostate cancer. Eur J Med Chem. 2026;308:118681. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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