PROTAC EGFR degrader 7
Based on 1 Customer Validation
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research. PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(Pink: ligand (HY-153605); Blue: Cereblon ligand (HY-A0003); Black: linker).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.85%
- CAS No.: 3033297-59-2
- Formule: C46H48N10O6
- Masse moléculaire:836.94
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Stockage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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EGFRL858R/T790M 13.2 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>100 μM
Compound: 13b
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Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
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[PMID: 35691176] |
| HCC827 | IC50 |
1.12 μM
Compound: 13b
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Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay
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[PMID: 35691176] |
| NCI-H1299 | IC50 |
>100 μM
Compound: 13b
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Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
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[PMID: 35691176] |
| NCI-H1975 | IC50 |
0.0468 μM
Compound: 13b
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Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay
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[PMID: 35691176] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Protocol for Cell Cycle
- Subcutaneous Cell-Line-Derived Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 3033297-59-2
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Appearance Solid
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Masse moléculaire 836.94
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Formule C46H48N10O6
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Color Off-white to light yellow
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SMILES
C#CCN(CCN(C1=CC(OC)=C(C=C1NC(C=C)=O)NC2=NC(C3=CN(C4=CC=CC=C34)C)=CC=N2)C)CCCC(NC5=C6CN(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O
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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 and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (119.48 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 and light). 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 and light). 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 (273 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
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 and light). 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 | 1.1948 mL | 5.9741 mL | 11.9483 mL | 29.8707 mL |
| 5 mM | 0.2390 mL | 1.1948 mL | 2.3897 mL | 5.9741 mL | |
| 10 mM | 0.1195 mL | 0.5974 mL | 1.1948 mL | 2.9871 mL | |
| 15 mM | 0.0797 mL | 0.3983 mL | 0.7966 mL | 1.9914 mL | |
| 20 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4935 mL | |
| 25 mM | 0.0478 mL | 0.2390 mL | 0.4779 mL | 1.1948 mL | |
| 30 mM | 0.0398 mL | 0.1991 mL | 0.3983 mL | 0.9957 mL | |
| 40 mM | 0.0299 mL | 0.1494 mL | 0.2987 mL | 0.7468 mL | |
| 50 mM | 0.0239 mL | 0.1195 mL | 0.2390 mL | 0.5974 mL | |
| 60 mM | 0.0199 mL | 0.0996 mL | 0.1991 mL | 0.4978 mL | |
| 80 mM | 0.0149 mL | 0.0747 mL | 0.1494 mL | 0.3734 mL | |
| 100 mM | 0.0119 mL | 0.0597 mL | 0.1195 mL | 0.2987 mL |
PROTAC EGFR degrader 7 Related Classifications
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