H3B-5942
Based on 1 Customer Validation
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.25%
- No. CAS: 2052128-15-9
- Fòrmula: C31H34N4O2
- Peso molecular:494.63
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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ERαY537S 0.41 nM (Ki) |
ERαWT 1 nM (Ki) |
H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively[1].
H3B-5942 elevates ERα protein level distinct from SERMs/SERD, blocks ERα-dependent transcription in breast cancer cells. H3B-5942 (0.01-10 μM) reduces ERα target gene GREB1 in MCF7-ERαWT, various MCF7-ERαMUT lines, and the PDX-ERαY537S/WT line[1].
H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERαWT, and MCF7-LTED-ERαY537C lines with GI50s of 0.5, 2, and 30 nM, respectively. H3B-5942 (10-25 nM) in combination with CDK4/6 inhibitors (≥25 pM) has synergic inhibitory effect on multiple cell lines bearing ERαWT or clinically frequent ERα mutations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
H3B-5942 (3, 10, 30, 100, and 200 mg/kg, p.o, q.d.) exhibits similar anti-tumor activity in the ERαY537S/WT ST941 model in athymic female nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MCF7 xenograft model in athymic female nude mice[1]
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Dosage:1, 3, 10, or 30 mg/kg
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Administration:P.O. once a day (q.d.×1) for 17 days
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Result:Exhibited tumor growth inhibition (TGI) on day 17 of 19%, 41%, 68%, and 83%, respectively.
Chemical Information
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No. CAS 2052128-15-9
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Appearance Solid
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Peso molecular 494.63
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Fòrmula C31H34N4O2
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Color White to off-white
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SMILES
CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCNC/C=C/C(N(C)C)=O)C=C2)\C3=CC(C=NN4)=C4C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 83.33 mg/mL (168.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0217 mL | 10.1086 mL | 20.2171 mL | 50.5428 mL |
| 5 mM | 0.4043 mL | 2.0217 mL | 4.0434 mL | 10.1086 mL | |
| 10 mM | 0.2022 mL | 1.0109 mL | 2.0217 mL | 5.0543 mL | |
| 15 mM | 0.1348 mL | 0.6739 mL | 1.3478 mL | 3.3695 mL | |
| 20 mM | 0.1011 mL | 0.5054 mL | 1.0109 mL | 2.5271 mL | |
| 25 mM | 0.0809 mL | 0.4043 mL | 0.8087 mL | 2.0217 mL | |
| 30 mM | 0.0674 mL | 0.3370 mL | 0.6739 mL | 1.6848 mL | |
| 40 mM | 0.0505 mL | 0.2527 mL | 0.5054 mL | 1.2636 mL | |
| 50 mM | 0.0404 mL | 0.2022 mL | 0.4043 mL | 1.0109 mL | |
| 60 mM | 0.0337 mL | 0.1685 mL | 0.3370 mL | 0.8424 mL | |
| 80 mM | 0.0253 mL | 0.1264 mL | 0.2527 mL | 0.6318 mL | |
| 100 mM | 0.0202 mL | 0.1011 mL | 0.2022 mL | 0.5054 mL |
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