Art. -Nr.: HY-153468

ErSO-TFPy

(Synonyms: TEQ103; Sera2)

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ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer.

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Reinheit: 99.33%
CAS. Nr.: 3035547-78-2
Formel: C₁₉H₁₃F₇N₂O₂
Molecular Weight:434.31

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ErSO-TFPy Chemical Structure

CAS. Nr.: 3035547-78-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

TRPM4

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	15 μM Compound: (R)-26	Anticancer activity against ERalpha negative human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue assay Anticancer activity against ERalpha negative human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue assay	[PMID: 35080871]
HCT-116	IC₅₀	24 μM Compound: (R)-26	Anticancer activity against ERalpha negative human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs by alamar blue assay Anticancer activity against ERalpha negative human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs by alamar blue assay	[PMID: 35080871]
HT-29	IC₅₀	15 μM Compound: (R)-26	Anticancer activity against ERalpha negative human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue assay Anticancer activity against ERalpha negative human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue assay	[PMID: 35080871]
HT-29	IC₅₀	25 μM Compound: (R)-26	Anticancer activity against ERalpha negative human HT-29 cells assessed as cell growth inhibition incubated for 24 hrs by alamar blue assay Anticancer activity against ERalpha negative human HT-29 cells assessed as cell growth inhibition incubated for 24 hrs by alamar blue assay	[PMID: 35080871]
MCF7	IC₅₀	0.004 μM Compound: (R)-26	Anticancer activity against ERalpha positive human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue assay Anticancer activity against ERalpha positive human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue assay	[PMID: 35080871]
MCF7	IC₅₀	0.005 μM Compound: (R)-26	Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 24 hrs by alamar blue assay Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 24 hrs by alamar blue assay	[PMID: 35080871]
MDA-MB-231	IC₅₀	14 μM Compound: (R)-26	Anticancer activity against ERalpha negative human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue assay Anticancer activity against ERalpha negative human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue assay	[PMID: 35080871]
MDA-MB-231	IC₅₀	22 μM Compound: (R)-26	Anticancer activity against ERalpha negative human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by alamar blue assay Anticancer activity against ERalpha negative human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by alamar blue assay	[PMID: 35080871]

In Vitro

ErSO-TFPy (72 h) potently inhibits viability of ERα-positive human breast cancer cell lines, with IC₅₀ values of ~5-25 nM after 72 h incubation, and has minimal activity against ERα-negative human breast cancer cell lines^[2].
ErSO-TFPy (150-450 nM; 6 h) activates the anticipatory unfolded protein response in MCF-7 human breast cancer cells at 150 and 450 nM after 6 h incubation, as measured by increased phosphorylation of EIF2α, increased phosphorylation of AMPK, and cleavage of ATF6^[2].
ErSO-TFPy (≥0.01 μM; 72 h) induces potent TRPM4-dependent cell death in MCF-7 human breast cancer cells, with ~80% cell death at concentrations ≥0.01 μM after 72 h incubation, while MCF-7 TRPM4 KO cells show ~1000-fold reduced sensitivity to ErSO-TFPy-induced cell death^[2].
ErSO-TFPy (1 μM; 2 h) induces significant TRPM4-dependent cell swelling in MCF-7 Parental human breast cancer cells at 1 μM after 2 h incubation, while MCF-7 TRPM4 KO cells show no measurable cell swelling^[2].
ErSO-TFPy (24-120 h) potently inhibits viability of MCF-7, MCF-7^Y537S mutant, and MCF-7^D538G mutant human breast cancer cells, with single-digit nanomolar IC₅₀ values after 24 and 120 h incubation under both 10% FBS and 10% CD-FBS + 1 nM E₂ media conditions^[2].

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

Western Blot Analysis^[2]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

150 nM, 450 nM
Incubation Time:

6 h
Result:

Induced activation of anticipatory unfolded protein response markers, including phosphorylation of EIF2α, phosphorylation of AMPK, and cleavage of ATF6.

Cell Viability Assay^[2]

Cell Line:

MCF-7 Parental and MCF-7 TRPM4 KO human breast cancer cells
Concentration:

≥0.01 μM (MCF-7 Parental; 72 h); 100 μM (MCF-7 TRPM4 KO; 168 h)
Incubation Time:

24 h, 72 h, 168 h
Result:

Induced ~80% cell death in MCF-7 Parental cells at concentrations ≥0.01 μM after 72 h. Reduced cell death induction by ~1000-fold in MCF-7 TRPM4 KO cells, with minimal cell death observed even at 100 μM after 168 h.

Cell Viability Assay^[2]

Cell Line:

MCF-7, MCF-7 Y537S mutant, and MCF-7 D538G mutant human breast cancer cells
Concentration:

4-8 nM (24 h); 4-8 nM (120 h)
Incubation Time:

24 h, 120 h
Result:

Exhibited single-digit nanomolar IC₅₀ values in 10% FBS media: 8 nM (24 h), 5 nM (120 h) in MCF-7 cells; 5 nM (24 h), 4 nM (120 h) in MCF-7 Y537S cells; 6 nM (24 h), 6 nM (120 h) in MCF-7 D538G cells. Exhibited single-digit nanomolar IC₅₀ values in 10% CD-FBS + 1 nM E2 media: 7nM (24 h), 6 nM (120 h) in MCF-7 cells; 4 ± 1 nM (24 h), 6 nM (120 h) in MCF-7 Y537S cells; 5 nM (24 h), 8 nM (120 h) in MCF-7 D538G cells.

Cell Cytotoxicity Assay^[2]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

50 nM
Incubation Time:

24 h, 120 h
Result:

Induced ~80% cell death at 50 nM after 24 h incubation. Induced ~80% cell death at 50 nM after 120 h incubation.

Parmacokinetics

Species	Dose	Route	Plasma Concentration
Mice^[1]	5 mg/kg	i.v.	7.25 ng/mL
Mice^[1]	20 mg/kg	i.v.	16.7 ng/mL
Mice^[1]	75 mg/kg	i.v.	178 ng/mL

In Vivo

ErSO-TFPy (TEQ103) (1-150 mg/kg total dose; i.v.) exhibits significant, durable antitumor activity in MCF-7 tumor-bearing athymic female mice, with 100% tumor-free survivors achieved regardless of administration schedule^[1].
ErSO-TFPy (2-10 mg/kg; i.v.; once weekly; 4 doses) induces complete regression of MCF-7 ERα+ breast cancer xenografts in athymic nude mice at 10 mg/kg, with significant tumor growth inhibition at 5 mg/kg, no significant inhibition at 2 mg/kg, and no significant weight loss^[2].
ErSO-TFPy (20 mg/kg; i.v.; once or twice weekly; 4 doses) induces complete regression of Fulvestrant (HY-13636)-resistant ST941 ESR1^mut breast cancer PDX tumors in athymic nude mice^[2].
ErSO-TFPy (2-50 mg/kg; i.v.; single dose) induces near-complete or complete regression of MCF-7 ESR1^D538G breast cancer xenografts, including large ~1500 mm³ tumors, in athymic nude mice at 25 mg/kg or 50 mg/kg, with significant inhibition at 5 mg/kg and no significant inhibition at 2 mg/kg^[2].
ErSO-TFPy (50 mg/kg; i.v.; single dose) induces significant regression of BT-474 ERα+/HER2+ breast cancer xenografts, including large established tumors, in athymic nude mice^[2].
ErSO-TFPy (50 mg/kg; i.v.; single dose) induces rapid necrotic cell death in MCF-7 ESR1^D538G breast cancer xenografts, with >90% tumor necrosis observed 3 to 5 days post-treatment, and no significant early involvement of assessed immune cell populations in tumor cell death^[2].

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

Animal Model:

Athymic (female; bearing ~500 mm3 subcutaneous MCF-7 tumors)^[1]
Dosage:

1 mg/kg, 2 mg/kg, 4 mg/kg, 15 mg/kg, 30 mg/kg; 1 mg/kg, 5 mg/kg, 20 mg/kg, 75 mg/kg, 150 mg/kg (intermittent schedule, day 1 and day 10)
Administration:

i.v.; daily for 10 days (daily schedule); i.v.; single doses on day 1 and day 10 (intermittent schedule)
Result:

Achieved 2/9 tumor-free survivors and a 44-day tumor growth delay in relapsing mice with 2 mg/kg daily schedule. Achieved 4/9 tumor-free survivors and a 56-day tumor growth delay in relapsing mice with 5 mg/kg intermittent schedule. Induced 100% tumor-free survivors with complete regressions lasting 121 days post-tumor induction at total dosages ≥40 mg/kg across both schedules. Caused no body weight loss in all studied dose ranges.

Animal Model:

Athymic nude mice (female, with exogenous estradiol pellet)^[2]
Dosage:

2 mg/kg; 5 mg/kg; 10 mg/kg
Administration:

i.v.; once weekly; 4 doses
Result:

Showed no significant tumor growth inhibition relative to vehicle at 2 mg/kg.\nInduced significant tumor growth inhibition at 5 mg/kg.\nInduced complete tumor regression at 10 mg/kg.\nCaused no significant weight loss in any treatment group.

Animal Model:

Athymic nude mice^[2]
Dosage:

20 mg/kg
Administration:

i.v.; once weekly; 4 doses; i.v.; twice weekly; 4 doses
Result:

Induced complete tumor regression in all 8 treated mice with both administration schedules.\nCaused significant reduction in tumor volume relative to vehicle with both administration schedules.

Animal Model:

Athymic nude mice (female)^[2]
Dosage:

2 mg/kg; 5 mg/kg; 25 mg/kg; 50 mg/kg
Administration:

i.v.; single dose (day 0); i.v.; single dose (day 53)
Result:

Showed no significant tumor growth inhibition at 2 mg/kg.\nInduced significant tumor growth inhibition at 5 mg/kg.\nInduced >80% tumor volume reduction within 14 days at 25 mg/kg and 50 mg/kg.\nResulted in 5/5 mice having no measurable tumors by day 66 at 50 mg/kg.\nInduced >90% tumor regression in ~1500 mm3 tumors treated with 50 mg/kg at day 53.

Animal Model:

Athymic nude mice (implanted with 0.5 mg 90-day release estrogen pellet)^[2]
Dosage:

50 mg/kg
Administration:

i.v.; single dose (day 0); i.v.; single dose (day 28)
Result:

Induced >80% tumor volume reduction within 14 days, with tumors continuing to regress through day 35, when treated at day 0.\nCaused significant tumor regression in large tumors treated at day 28.

Animal Model:

Athymic nude mice (female)^[2]
Dosage:

50 mg/kg
Administration:

i.v.; single dose
Result:

Induced degenerative state in tumors by day 1 post-treatment.\nCaused >90% of tumor tissue to be necrotic by days 3 and 5 post-treatment.\nReduced Ki67+ proliferative cells and cleaved caspase-3+ apoptotic cells significantly relative to vehicle in day 1 tumor tissue.\nCaused no significant difference in Ly6G+ neutrophils, CD11c+ dendritic cells, or F4/80+ macrophages in viable tumor regions relative to vehicle.

Chemical Information

CAS. Nr. 3035547-78-2
Appearance Solid
Molecular Weight 434.31
Formel C₁₉H₁₃F₇N₂O₂
Color White to off-white
SMILES

O=C1[C@@](N2CC(F)(C(F)(C2)F)F)(C3=CC=C(C=C3)O)C4=CC=CC(C(F)(F)F)=C4N1
Synonyms

TEQ103; Sera2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (230.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3025 mL

11.5125 mL

23.0250 mL

5 mM

0.4605 mL

2.3025 mL

4.6050 mL

10 mM

0.2303 mL

1.1513 mL

2.3025 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (11.51 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (11.51 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 5 mg/mL (11.51 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (291 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Marie-Christine Bissery, et al. Abstract 5629_ TEQ103, a novel therapeutic for the treatment of estrogen receptor alpha positive (ERα+) breast cancer. Cancer Res (2025) 85 (8_Supplement_1): 5629.

[2]. Mulligan MP, et al. Single Dose of a Small Molecule Leads to Complete Regressions of Large Breast Tumors in Mice. ACS Cent Sci. 2025;11(2):228-238. Published 2025 Jan 22. [Content Brief]

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.

Complete Stock Solution Preparation Table

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	2.3025 mL	11.5125 mL	23.0250 mL	57.5626 mL
	5 mM	0.4605 mL	2.3025 mL	4.6050 mL	11.5125 mL
	10 mM	0.2303 mL	1.1513 mL	2.3025 mL	5.7563 mL
	15 mM	0.1535 mL	0.7675 mL	1.5350 mL	3.8375 mL
	20 mM	0.1151 mL	0.5756 mL	1.1513 mL	2.8781 mL
	25 mM	0.0921 mL	0.4605 mL	0.9210 mL	2.3025 mL
	30 mM	0.0768 mL	0.3838 mL	0.7675 mL	1.9188 mL
	40 mM	0.0576 mL	0.2878 mL	0.5756 mL	1.4391 mL
	50 mM	0.0461 mL	0.2303 mL	0.4605 mL	1.1513 mL
	60 mM	0.0384 mL	0.1919 mL	0.3838 mL	0.9594 mL
	80 mM	0.0288 mL	0.1439 mL	0.2878 mL	0.7195 mL
	100 mM	0.0230 mL	0.1151 mL	0.2303 mL	0.5756 mL

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ErSO-TFPy

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Anti-Breast Cancer Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ErSO-TFPy

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Anti-Breast Cancer Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ErSO-TFPy Related Classifications

HY-153468 Related Classifications