PROTAC EGFR degrader 2
Based on 1 Customer Validation
PROTAC EGFR degrader 2 is an EGFR-targeting PROTAC and antitumor agent. PROTAC EGFR degrader 2 induces degradation of EGFR protein via the ubiquitin-proteasome system, requiring binding to both EGFR and the VHL E3 ubiquitin ligase. PROTAC EGFR degrader 2 exerts antitumor efficacy following EGFR degradation. PROTAC EGFR degrader 2 is released from the NTR-responsive caged-PROTAC 17-1 upon activation by nitroreductase in hypoxic tumor tissues. PROTAC EGFR degrader 2 can be used for the research of non-small cell lung cancer.
(Pink: EGFR ligand (HY-13272); Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- Purity: 95.09%
- CAS No.: 3031336-58-7
- Formula: C58H72ClFN12O8S
- Molecular Weight:1151.78
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
EGFR 36.51 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC827 | IC50 |
4.0 nM
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Antiproliferative activity against human HCC-827 cells under normoxic conditions incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against human HCC-827 cells under normoxic conditions incubated for 72 hrs by CCK8 assay.
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35175763 |
| HCC827 | DC50 |
36.51 nM
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EGFR degradation activity in human HCC-827 cells.
EGFR degradation activity in human HCC-827 cells.
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35175763 |
| HCC827 | IC50 |
6.0 nM
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Antiproliferative activity against human HCC-827 cells under normoxic conditions with exogenous 8 μg/mL NTR incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against human HCC-827 cells under normoxic conditions with exogenous 8 μg/mL NTR incubated for 72 hrs by CCK8 assay.
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35175763 |
| HCC827 | IC50 |
18.7 nM
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Antiproliferative activity against human HCC-827 cells under hypoxic conditions (<1% O2) incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against human HCC-827 cells under hypoxic conditions (<1% O2) incubated for 72 hrs by CCK8 assay.
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35175763 |
In Vitro
PROTAC EGFR degrader 2 (compound 17) potently inhibits the proliferation of HCC-827 cells, with an IC50 value of 4.0 nM[1].
PROTAC EGFR degrader 2 (50-500 nM; 72 h) induces concentration-dependent degradation of EGFR protein in HCC-827 cells under normoxic conditions[1].
PROTAC EGFR degrader 2 induces EGFR degradation in HCC-827 cells with a DC50 of 36.51 nM[1].
PROTAC EGFR degrader 2 (72 h) potently inhibits the proliferation of HCC-827 cells under normoxic conditions (with exogenous addition of 8 μg/mL NTR) with an IC50 value of 6.0 nM; it also inhibits the proliferation of HCC-827 cells under hypoxic conditions (< 1% O2) with an IC50 value of 18.7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC-827 cells
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Concentration:50, 100, 250, 500 nM
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Incubation Time:72 h
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Result:Induced EGFR degradation in HCC-827 cells in a concentration-dependent manner, with reduced EGFR protein levels observed at all tested concentrations relative to DMSO control.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3031336-58-7
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Appearance Solid
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Molecular Weight 1151.78
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Formula C58H72ClFN12O8S
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Color Light yellow to yellow
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SMILES
FC(C=CC(NC1=NC=NC2=CC(OCCCCCC3=CN(N=N3)CCOCCOCC(N[C@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)C(C)(C)C)=O)=C(C=C21)NC(/C=C/CN7CCCCC7)=O)=C8)=C8Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (86.82 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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:
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: ≥ 2.5 mg/mL (2.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (280 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 (protect from light, stored under nitrogen). 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 | 0.8682 mL | 4.3411 mL | 8.6822 mL | 21.7055 mL |
| 5 mM | 0.1736 mL | 0.8682 mL | 1.7364 mL | 4.3411 mL | |
| 10 mM | 0.0868 mL | 0.4341 mL | 0.8682 mL | 2.1706 mL | |
| 15 mM | 0.0579 mL | 0.2894 mL | 0.5788 mL | 1.4470 mL | |
| 20 mM | 0.0434 mL | 0.2171 mL | 0.4341 mL | 1.0853 mL | |
| 25 mM | 0.0347 mL | 0.1736 mL | 0.3473 mL | 0.8682 mL | |
| 30 mM | 0.0289 mL | 0.1447 mL | 0.2894 mL | 0.7235 mL | |
| 40 mM | 0.0217 mL | 0.1085 mL | 0.2171 mL | 0.5426 mL | |
| 50 mM | 0.0174 mL | 0.0868 mL | 0.1736 mL | 0.4341 mL | |
| 60 mM | 0.0145 mL | 0.0724 mL | 0.1447 mL | 0.3618 mL | |
| 80 mM | 0.0109 mL | 0.0543 mL | 0.1085 mL | 0.2713 mL |
PROTAC EGFR degrader 2 Related Classifications
HY-144304 Related Classifications
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