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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 channelTRPM4, 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.
For research use only. We do not sell to patients.
ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channelTRPM4, 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[1][2].
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-7Y537S mutant, and MCF-7D538G 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.
Induced activation of anticipatory unfolded protein response markers, including phosphorylation of EIF2α, phosphorylation of AMPK, and cleavage of ATF6.
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.
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 ESR1mut 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 ESR1D538G 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 ESR1D538G 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.
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.
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.
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.
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.
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.
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 (230.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
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
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.
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.
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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 μLDMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 μLDMSO stock solution (50.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
*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.
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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