X15695

Cat. No.: HY-175785: Data Sheet Handling Instructions
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X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer.

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

X15695 Chemical Structure

CAS No. : 353258-25-0

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View All Estrogen Receptor/ERR Isoform Specific Products:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

ERα

In Vitro

X15695 inhibits MCF-7, MC7^D538G and MC7^Y537S cells proliferation with IC₅₀s of 0.7, 74.42 and 0.38 nM, and the IC₅₀ values in the presence of estrogen (E2) are 10.28, 48.01 and 10.78 nM, respectively^[1].
X15695 inhibits MCF-7 cells colony growth when the activity of AHR is blocked with CH223191 (HY-12684) ^[1].
X15695 (1-10 μM, 7 days) inhibits the growth of organoids from patient-derived xenograft tumours (PDxO) ^[1].
X15695 (1 μM, 48 h) blocks cell cycle and induces apoptosis in MCF-7 cells, T47D cells, LNCaP cells and LAPC-4 cells by activating wild-type p53 and disrupting the gain-of-function tumorigenic activity of mutant p53, respectively^[2].

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

Apoptosis Analysis^[2]

Cell Line:	MCF-7 cells, T47D cells, LNCaP cells and LAPC-4 cells
Concentration:	1 μM
Incubation Time:	48 h
Result:	Induced apoptosis in ER+ breast cancer cells, and the apoptotic effect was more significant in wild-type p53 cells.

Cell Cycle Analysis^[2]

Cell Line:	MCF-7 cells, T47D cells, LNCaP cells and LAPC-4 cells
Concentration:	1 μM
Incubation Time:	48 h
Result:	Significantly arrested the cells in the G1 phase in MCF-7 cells and G2/M phase in T47D cells. Induced G1/S phase arrest in the LNCaP cells and a G2/M arrest in the LAPC-4 cells.

Western Blot Analysis^[2]

Cell Line:	MCF-7 cells and T47D cells
Concentration:	1 μM
Incubation Time:	48 h
Result:	Significantly increase the level of p53 protein in MCF-7 cells. Had no significant impact in T47D cells.

In Vivo

X15695 (15-30 mg/kg, i.g., once daily for 16-42 days) potently inhibits the growth of breast tumor but less efficiently the growth of prostate tumor in mice^[2].

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

Animal Model:	MCF-7 and LAPC-4 cells induced xenograft model established in 6–7weeks old female(for MCF-7 cells) and male (forLAPC-4cells) athymic nude-Foxn1^nu mice (Envigo 6901M)^[2
Dosage:	30 mg/kg for MCF-7 model; 15 and 30 mg/kg for LAPC-4 model
Administration:	Oal gavage (i.g), once daily for 16 days (MCF-7 model) or 42 days (LAPC-4 model)
Result:	Significantly inhibits tumor growth, without weight loss or other toxic signs in MCF-7 model. Downregulated ERα and upregulated p53 in tumor tissue. Inhibited the growth of prostate tumors (30 mg/kg), but the effect was relatively weak.

Molecular Weight

314.67

Formula

C₁₄H₇ClF₄N₂

CAS No.

353258-25-0

SMILES

FC(C1=CN2C(C(Cl)=C1)=NC(C3=CC=C(F)C=C3)=C2)(F)F

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]. Katrin Koellisch, et al. Distinct 2-phenyl-imidazo[1, 2α] pyridine derivatives drive ER degradation and selectively impair proliferation of ER breast cancer cells via the aryl hydrocarbon receptor+. 2025 Aug 1

[2]. Pan M, et al. Identification of an Imidazopyridine-based Compound as an Oral Selective Estrogen Receptor Degrader for Breast Cancer Therapy. Cancer Res Commun. 2023 Jul 27;3(7):1378-1396.

X15695 Related Classifications

Cancer

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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.

Keywords:

X15695353258-25-0X 15695X-15695Estrogen Receptor/ERRAryl Hydrocarbon ReceptorApoptosisMDM-2/p53AhRMCF-7 cellsT47D cellsLNCaP cellsLAPC-4 cellsPatient-derived xenograft tumoursmice modelInhibitorinhibitorinhibit

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