PROTAC EZH2 Degrader-1
Based on 2 publication(s) in Google Scholar
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes.
(Pink: EZH2 ligand (HY-147230); Blue: Cereblon ligand (HY-103596); Black: linker).
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- Pureté : 99.44%
- CAS No.: 2641601-67-2
- Formule: C54H67N7O8
- Masse moléculaire:942.15
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PROTAC EZH2 Degrader-1
MoreVoir tous les produits spécifiques à Isoform PROTACs
MoreVoir tous les produits spécifiques à Isoform Histone Methyltransferase
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Activité biologique
Description
IC50 & Target
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EZH2 2.7 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EOL1 | IC50 |
3.7 μM
Compound: E7
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Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
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[PMID: 38295690] |
| MV4-11 | IC50 |
5.5 μM
Compound: E7
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Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
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[PMID: 38295690] |
| Pfeiffer | IC50 |
0.21 μM
Compound: E7
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Antiproliferative activity against human Pfeiffer cells harboring EZH2-A677G mutant assessed as inhibition of cell growth incubated for 3 to 7 days by optical microscopic analysis (Rvb= 0.49 uM)
Antiproliferative activity against human Pfeiffer cells harboring EZH2-A677G mutant assessed as inhibition of cell growth incubated for 3 to 7 days by optical microscopic analysis (Rvb= 0.49 uM)
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[PMID: 33606537] |
| RS4-11 | IC50 |
5 μM
Compound: E7
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Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
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[PMID: 38295690] |
| WSUDLCL2 | IC50 |
3.69 μM
Compound: E7
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Antiproliferative activity against human WSUDLCL2 cells harboring EZH2-Y641F mutant assessed as inhibition of cell growth incubated for 3 to 7 days by optical microscopic analysis (Rvb= 4.92 uM)
Antiproliferative activity against human WSUDLCL2 cells harboring EZH2-Y641F mutant assessed as inhibition of cell growth incubated for 3 to 7 days by optical microscopic analysis (Rvb= 4.92 uM)
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[PMID: 33606537] |
In Vitro
PROTAC EZH2 Degrader-1 inhibits the cell viability of cells H128-LM (isolated from leptomeningeal metastasis), H128-BPM (isolated from brain parenchymal metastasis), H128 wildtype and H128-Mut with IC50s of 1.83 nM, 1.9 nM, 3.07 nM and 2.64 nM, respectively[2].
PROTAC EZH2 Degrader-1 enhances the sensitivity of H128-LM cells to Carboplatin (HY-17393), VP16 (HY-13629) and VM26 (HY-13761)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H128
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Concentration:0-10 nM
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Incubation Time:72 h
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Result:Inhibited the cell viability.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:H128-LM xenograft mouse models[2]
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Dosage:0.5 mg/kg
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Administration:ip, once weekly for 3 doses
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Result:Inhibited the tumor growth and prolonged the survival time when combined with Carboplatin, VP16 or VM26.
Chemical Information
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CAS No. 2641601-67-2
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Appearance Solid
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Masse moléculaire 942.15
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Formule C54H67N7O8
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Color Off-white to light yellow
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SMILES
CCN(C1CCOCC1)C2=C(C(C(NCC3=C(C=C(NC3=O)C)C)=O)=CC(C4=CC=C(C=C4)CN5CCN(CC5)CCCCCCCOC6=C7C(N(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)=C2)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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BMC Cancer
PROTAC EZH2 degrader-1 overcomes the resistance of podophyllotoxin derivatives in refractory small cell lung cancer with leptomeningeal metastasis. [Abstract]2024 Apr 22;24(1):504. PMID: 38644473 -
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (106.14 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (275 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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Instruction de manipulation (2659 KB)
Références
[1]. Juan Xia, et al. Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects. J Med Chem. 2022 May 26;65(10):7016-7043. [Content Brief]
[2]. Shi MX, et al., PROTAC EZH2 degrader-1 overcomes the resistance of podophyllotoxin derivatives in refractory small cell lung cancer with leptomeningeal metastasis. BMC Cancer. 2024 Apr 22;24(1):504. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.0614 mL | 5.3070 mL | 10.6140 mL | 26.5351 mL |
| 5 mM | 0.2123 mL | 1.0614 mL | 2.1228 mL | 5.3070 mL | |
| 10 mM | 0.1061 mL | 0.5307 mL | 1.0614 mL | 2.6535 mL | |
| 15 mM | 0.0708 mL | 0.3538 mL | 0.7076 mL | 1.7690 mL | |
| 20 mM | 0.0531 mL | 0.2654 mL | 0.5307 mL | 1.3268 mL | |
| 25 mM | 0.0425 mL | 0.2123 mL | 0.4246 mL | 1.0614 mL | |
| 30 mM | 0.0354 mL | 0.1769 mL | 0.3538 mL | 0.8845 mL | |
| 40 mM | 0.0265 mL | 0.1327 mL | 0.2654 mL | 0.6634 mL | |
| 50 mM | 0.0212 mL | 0.1061 mL | 0.2123 mL | 0.5307 mL | |
| 60 mM | 0.0177 mL | 0.0885 mL | 0.1769 mL | 0.4423 mL | |
| 80 mM | 0.0133 mL | 0.0663 mL | 0.1327 mL | 0.3317 mL | |
| 100 mM | 0.0106 mL | 0.0531 mL | 0.1061 mL | 0.2654 mL |
PROTAC EZH2 Degrader-1 Related Classifications
HY-147525 Related Classifications
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