PROTAC EGFR degrader 4
Based on 1 Customer Validation
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
(Pink: EGFRdel19 and EGFRL858R/T790M Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker (HY-W007714)).
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 2882845-50-1
- Formula: C55H70N12O4S
- Molecular Weight:995.29
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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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EGFRL858R/T790M |
EGFRdel19 |
VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
245 nM
Compound: P3
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Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
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[PMID: 32883633] |
| HCC827 | IC50 |
0.76 nM
Compound: P3
|
Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 32883633] |
| HCC827 | IC50 |
0.76 nM
Compound: 4
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Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation
Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation
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[PMID: 35254067] |
| HepG2 | IC50 |
>5000 nM
Compound: P3
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Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 72 hrs by MTT assay
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[PMID: 32883633] |
| NCI-H1975 | IC50 |
203 nM
Compound: P3
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Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
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[PMID: 32883633] |
| NCI-H1975 | IC50 |
203 nM
Compound: 4
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Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation
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[PMID: 35254067] |
PROTAC EGFR degrader 4 (compound P3) has antiproliferative activity against cancer cells A431 (EGFR WT), HCC827 (EGFRdel19) and H1975 (EGFRL858R/T790M) with IC50s of 245 ± 30 nM, 0.83 ± 0.30 nM and 203 ± 21 nM, respectively[1].
PROTAC EGFR degrader 4 (0.3-100 nM; 48 hours) displays excellent activity of inducing EGFRdel19 degradation with a DC50 values of 0.51 nM[1].
PROTAC EGFR degrader 4 (3 and 100 nM; 48 hours) dramatically reduces the phosphorylation of EGFR and its downstream effector Akt in HCC827 and H1975 cell lines[1].
PROTAC EGFR degrader 4 (10 and 100 nM; 48 hours) induces 31.07% and 44.80% of HCC827 cell line to undergo apoptosis at concentration of 10 and 100 nM, respectively; and arrests both HCC827 and H1975 cell lines at G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2882845-50-1
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Appearance Solid
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Molecular Weight 995.29
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Formula C55H70N12O4S
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Color White to off-white
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SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCN4CCN(CC4)C5=CC=C(C=C5)NC6=NC=C7N=C(N(C7=N6)C8CCCC8)NC9=CC=CC=C9)=O)=O)O)=O
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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 (100.47 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)
Purity & Documentation
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Data Sheet (271 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 | 1.0047 mL | 5.0237 mL | 10.0473 mL | 25.1183 mL |
| 5 mM | 0.2009 mL | 1.0047 mL | 2.0095 mL | 5.0237 mL | |
| 10 mM | 0.1005 mL | 0.5024 mL | 1.0047 mL | 2.5118 mL | |
| 15 mM | 0.0670 mL | 0.3349 mL | 0.6698 mL | 1.6746 mL | |
| 20 mM | 0.0502 mL | 0.2512 mL | 0.5024 mL | 1.2559 mL | |
| 25 mM | 0.0402 mL | 0.2009 mL | 0.4019 mL | 1.0047 mL | |
| 30 mM | 0.0335 mL | 0.1675 mL | 0.3349 mL | 0.8373 mL | |
| 40 mM | 0.0251 mL | 0.1256 mL | 0.2512 mL | 0.6280 mL | |
| 50 mM | 0.0201 mL | 0.1005 mL | 0.2009 mL | 0.5024 mL | |
| 60 mM | 0.0167 mL | 0.0837 mL | 0.1675 mL | 0.4186 mL | |
| 80 mM | 0.0126 mL | 0.0628 mL | 0.1256 mL | 0.3140 mL | |
| 100 mM | 0.0100 mL | 0.0502 mL | 0.1005 mL | 0.2512 mL |
PROTAC EGFR degrader 4 Related Classifications
HY-146349 Related Classifications
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