2. Vitamin D Related/Nuclear Receptor Immunology/Inflammation Apoptosis
  3. Estrogen Receptor/ERR Aryl Hydrocarbon Receptor Apoptosis MDM-2/p53
  4. X15695

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.

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X15695

X15695 Chemical Structure

CAS No. : 353258-25-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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X15695 Related Antibodies

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Description

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[1][2].

IC50 & Target[1]

ERα

 

In Vitro

X15695 inhibits MCF-7, MC7D538G and MC7Y537S 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.

X15695 Related Antibodies

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-Foxn1nu 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.
Appearance

Solid

Color

Off-white to light yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (317.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1779 mL 15.8897 mL 31.7793 mL
5 mM 0.6356 mL 3.1779 mL 6.3559 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1779 mL 15.8897 mL 31.7793 mL 79.4483 mL
5 mM 0.6356 mL 3.1779 mL 6.3559 mL 15.8897 mL
10 mM 0.3178 mL 1.5890 mL 3.1779 mL 7.9448 mL
15 mM 0.2119 mL 1.0593 mL 2.1186 mL 5.2966 mL
20 mM 0.1589 mL 0.7945 mL 1.5890 mL 3.9724 mL
25 mM 0.1271 mL 0.6356 mL 1.2712 mL 3.1779 mL
30 mM 0.1059 mL 0.5297 mL 1.0593 mL 2.6483 mL
40 mM 0.0794 mL 0.3972 mL 0.7945 mL 1.9862 mL
50 mM 0.0636 mL 0.3178 mL 0.6356 mL 1.5890 mL
60 mM 0.0530 mL 0.2648 mL 0.5297 mL 1.3241 mL
80 mM 0.0397 mL 0.1986 mL 0.3972 mL 0.9931 mL
100 mM 0.0318 mL 0.1589 mL 0.3178 mL 0.7945 mL
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X15695 Related Classifications

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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