PROTAC EGFR degrader 2
Based on 1 Customer Validation
PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC.
(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
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EGFR 36.51 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
>20 μM
Compound: I-6
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Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
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[PMID: 38759458] |
| A549 | IC50 |
>20 μM
Compound: I-6
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Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
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[PMID: 38759458] |
| HCC827 | IC50 |
0.004 μM
Compound: I-6
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Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
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[PMID: 38759458] |
| HCC827 | IC50 |
18.7 nM
Compound: 17
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Antiproliferative activity against human HCC827 cells assessed as cell viability measured after 72 hrs under hypoxic condition by CCK-8 assay
Antiproliferative activity against human HCC827 cells assessed as cell viability measured after 72 hrs under hypoxic condition by CCK-8 assay
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[PMID: 35175763] |
| HCC827 | IC50 |
4 nM
Compound: 17
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Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs under normoxic condition by CCK-8 assay
Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs under normoxic condition by CCK-8 assay
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[PMID: 35175763] |
| HCC827 | IC50 |
6 nM
Compound: 17
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Antiproliferative activity against human HCC827 cells assessed as cell viability measured after 72 hrs in presence of NTR by CCK-8 assay
Antiproliferative activity against human HCC827 cells assessed as cell viability measured after 72 hrs in presence of NTR by CCK-8 assay
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[PMID: 35175763] |
| NCI-H1975 | IC50 |
1.93 μM
Compound: I-6
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
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[PMID: 38759458] |
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
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)
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.
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 (270 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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