PROTAC ERα Degrader-4
Based on 1 Customer Validation
PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
For research use only. We do not sell to patients.
- Purity: 98.63%
- CAS No.: 2521299-80-7
- Formula: C55H62F3N5O10S2
- Molecular Weight:1074.23
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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ERα 5.08 μM (Ki) |
ERβ 26.20 μM (Ki) |
PROTAC ERα Degrader-4 (1 μM, 12 hours) exhibits significant degradation activity for ERα in MCF-7cells[1].
PROTAC ERα Degrader-4 (2 μM, 12 hours) can degrade wild-type ERα inT47D cells and mutant ERα in T47DD538G and T47DY537S cells[1].
PROTAC ERα Degrader-4 (0.01-10 μM, 72 hours) has inhibitory activity of ERα in Tamoxifen (HY-13757A) -sensitive MCF-7 cells, with the IC50 value of 0.05 μM[1].
PROTAC ERα Degrader-4 (1-10 μM, 72 hours) induce apoptosis and cell cycle arrest of MCF-7 cells[1].
PROTAC ERα Degrader-4 (0.01-10 μM, 12 hours) efficiently degrades ERα protein in the range of 0.01 to10 μM in MCF-7 cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:0.01-10 μM
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Incubation Time:72 hours
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Result:Had inhibitory activity in Tamoxifen-sensitive MCF-7 cells, with the IC50 value of 0.05 μM.
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Cell Line:MCF-7 cells
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Concentration:1.0 μM, 5 μM, 5.0 μM
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Incubation Time:72 hours
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Result:Induced apoptosis.
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Cell Line:MCF-7 cells
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Concentration:0.01-10 μM
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Incubation Time:72 hours
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Result:Induced cell cycle arrest.
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Cell Line:MCF-7 cells
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Concentration:0.01-10 μM
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Incubation Time:12 hours
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Result:Efficiently degraded ERα protein in the range of 0.01 to10 μM, whereas ERα protein levels recovered slightly at a high concentration of 10 μM
PROTAC ERα Degrader-4 (5 mg/kg for i.v.) shows a T1/2 of 4.61 h and CL of 64.4 mL/min/kg[1].
Pharmacokinetic parameters for PROTAC ERα Degrader-4 (Compound ZD12) in BALB/C female mice[1]
| Route | Dose (mg/kg) | CL (mL/min/kg) | Tmax (h) | T1/2 (h) | Cmax (ng/mL) | AUC (h•ng/mL) |
| i.v. | 5 | 64.4 | 0.08 | 4.61 | 3635.73 | 1342 |
| p.o. | 20 | ND | ND | ND | ND | ND |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LCC2 orthotopic xenograft tumor models[1]
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Dosage:5 μM/kg
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Administration:Intravenous injection (i.p.)
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Result:Exhibited potent antitumor activity and ERα degradation effect in tumor tissues.
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Animal Model:BALB/C female mice (Pharmacokinetic assay)[1]
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Dosage:5 mg/kg; 20 mg/kg
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Administration:Intravenous injection (i.v.); Oral gavage (p.o.)
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Result:
Chemical Information
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CAS No. 2521299-80-7
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Appearance Solid
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Molecular Weight 1074.23
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Formula C55H62F3N5O10S2
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Color White to light yellow
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SMILES
O=[S](N(C(C=C1)=CC=C1OCCCCCC(N[C@@H](C(C)(C)C)C(N(C[C@@H]2O)[C@@H](C2)C(N[C@H](C3=CC=C(C(SC=N4)=C4C)C=C3)C)=O)=O)=O)CC(F)(F)F)(C5[C@@H]6C(C(C=C7)=CC=C7O)=C(C(C=C8)=CC=C8O)[C@H](C5)O6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (93.09 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, 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 | 0.9309 mL | 4.6545 mL | 9.3090 mL | 23.2725 mL |
| 5 mM | 0.1862 mL | 0.9309 mL | 1.8618 mL | 4.6545 mL | |
| 10 mM | 0.0931 mL | 0.4654 mL | 0.9309 mL | 2.3272 mL | |
| 15 mM | 0.0621 mL | 0.3103 mL | 0.6206 mL | 1.5515 mL | |
| 20 mM | 0.0465 mL | 0.2327 mL | 0.4654 mL | 1.1636 mL | |
| 25 mM | 0.0372 mL | 0.1862 mL | 0.3724 mL | 0.9309 mL | |
| 30 mM | 0.0310 mL | 0.1551 mL | 0.3103 mL | 0.7757 mL | |
| 40 mM | 0.0233 mL | 0.1164 mL | 0.2327 mL | 0.5818 mL | |
| 50 mM | 0.0186 mL | 0.0931 mL | 0.1862 mL | 0.4654 mL | |
| 60 mM | 0.0155 mL | 0.0776 mL | 0.1551 mL | 0.3879 mL | |
| 80 mM | 0.0116 mL | 0.0582 mL | 0.1164 mL | 0.2909 mL |
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