Art. -Nr.: HY-123921

Gefitinib-based PROTAC 3

Name: Gefitinib-based PROTAC 3
Brand: MedChemExpress
SKU: HY-123921
Price: 132.00 USD
Availability: InStock
Rating: 5 (4 reviews)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Gefitinib-based PROTAC 3 is a PROTAC degrader targeting EGFR, with a DC₅₀ of 11.7 nM against exon 19 deletion mutants and a DC₅₀ of 22.3 nM against EGFR^L858R. Gefitinib-based PROTAC 3 selectively induces the ubiquitin-proteasome degradation of exon 19 deletion-mutant and L858R-mutant EGFR by recruiting the VHL E3 ligase. Gefitinib-based PROTAC 3 can be used for the research of EGFR mutation-positive cancers.
(Pink: EGFR ligand (HY-79511); Blue: ligand (HY-125845); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.98%
CAS. Nr.: 2230821-27-7
Formel: C₄₇H₅₇ClFN₇O₈S
Molecular Weight:934.51

Speicherung:

4°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)

Gefitinib-based PROTAC 3 Chemical Structure

CAS. Nr.: 2230821-27-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Gefitinib-based PROTAC 3 is a PROTAC degrader targeting EGFR, with a DC₅₀ of 11.7 nM against exon 19 deletion mutants and a DC₅₀ of 22.3 nM against EGFR^L858R. Gefitinib-based PROTAC 3 selectively induces the ubiquitin-proteasome degradation of exon 19 deletion-mutant and L858R-mutant EGFR by recruiting the VHL E3 ligase. Gefitinib-based PROTAC 3 can be used for the research of EGFR mutation-positive cancers^[1]. (Pink: EGFR ligand (HY-79511); Blue: ligand (HY-125845); Black: linker).

IC₅₀ & Target

^[1]

EGFR

11.7 nM (DC₅₀, HCC827(exon 19 del) cells)

EGFR

22.3 nM (DC₅₀, H3255^L858Rcells)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC827	DC₅₀	11.7 nM	Half-maximal degradation concentration of exon 19 deletion mutant EGFR in human HCC827 cells assessed by immunoblot-based target degradation assay following 24 h incubation. Half-maximal degradation concentration of exon 19 deletion mutant EGFR in human HCC827 cells assessed by immunoblot-based target degradation assay following 24 h incubation.	29129716
NCI-H3255	DC₅₀	22.3 nM	Half-maximal degradation concentration of L858R mutant EGFR in human H3255 cells assessed by immunoblot-based target degradation assay following 24 h incubation. Half-maximal degradation concentration of L858R mutant EGFR in human H3255 cells assessed by immunoblot-based target degradation assay following 24 h incubation.	29129716

In Vitro

Gefitinib-based PROTAC 3 (compound 3) (100 nM-10 μM; 24 h) potently degrades exon 19 deletion-mutant EGFR in HCC827 cells, with a DC₅₀ of 11.7 nM and a maximum degradation rate of 98.9%^[1].
Gefitinib-based PROTAC 3 (25 nM-10 μM; 24 h) potently degrades EGFR^L858R in H3255 cells, with a DC₅₀ of 22.3 nM and a maximum degradation rate of 96.6%^[1].
Gefitinib-based PROTAC 3 (25 nM-10 μM; 24 h) exerts no effect on wild-type EGFR in OVCAR8 cells, and exhibits selective degradation activity against mutant EGFR subtypes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HCC827 cells
Concentration:

100, 250 nM; 1, 2.5, 10 μM
Incubation Time:

24 h
Result:

Potently degraded exon 19 deletion mutant EGFR in HCC827 cells with a DC₅₀ of 11.7 nM and achieves 98.9% maximum degradation.

Western Blot Analysis^[1]

Cell Line:

H3255 cells
Concentration:

25, 100, 250 nM; 1, 2.5, 10 μM
Incubation Time:

24 h
Result:

Potently degraded EGFR^L858R in H3255 cells with a DC₅₀of 22.3 nM and achieves 96.6% maximum degradation.

Western Blot Analysis^[1]

Cell Line:

OVCAR8 cells
Concentration:

25, 100, 250 nM; 1, 2.5, 10 μM
Incubation Time:

24 h
Result:

Exerted no effect on wild-type EGFR in OVCAR8 cells, and exhibited selective degradation activity against mutant EGFR subtypes.

Related Protocols :

Genotoxicity/Mutagenicity Study

Chemical Information

CAS. Nr. 2230821-27-7
Appearance Solid
Molecular Weight 934.51
Formel C₄₇H₅₇ClFN₇O₈S
Color Off-white to light yellow
SMILES

O=C([C@H]1N(C([C@@H](NC(CCOCCOCCCCCOC2=CC3=C(NC4=CC=C(F)C(Cl)=C4)N=CN=C3C=C2OC)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°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)

Publications (4)

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Journal Impact Factor

Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Drug Dev Res

Proteolysis targeting chimera (PROTAC) for epidermal growth factor receptor enhances anti-tumor immunity in non-small cell lung cancer. [Abstract]

2021 May;82(3):422-429. PMID: 33231319
J Biol Chem

Low-dose EGFR inhibition unlocks ferroptosis susceptibility to sensitize chemotherapy in EGFR-high triple-negative breast cancer. [Abstract]

2026 May 25:113185. PMID: 42190815
Int J Legal Med

Charting the growth through intelligence: A SWOC analysis on AI-assisted radiologic bone age estimation. [Abstract]

2025 Mar;139(2):679-694. PMID: 39460772

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 60 mg/mL (64.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0701 mL

5.3504 mL

10.7008 mL

5 mM

0.2140 mL

1.0701 mL

2.1402 mL

10 mM

0.1070 mL

0.5350 mL

1.0701 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (2.68 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.83 mg/mL (0.89 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell chemical biology. 2018 Jan 18;25(1):67-77.e3. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0701 mL	5.3504 mL	10.7008 mL	26.7520 mL
	5 mM	0.2140 mL	1.0701 mL	2.1402 mL	5.3504 mL
	10 mM	0.1070 mL	0.5350 mL	1.0701 mL	2.6752 mL
	15 mM	0.0713 mL	0.3567 mL	0.7134 mL	1.7835 mL
	20 mM	0.0535 mL	0.2675 mL	0.5350 mL	1.3376 mL
	25 mM	0.0428 mL	0.2140 mL	0.4280 mL	1.0701 mL
	30 mM	0.0357 mL	0.1783 mL	0.3567 mL	0.8917 mL
	40 mM	0.0268 mL	0.1338 mL	0.2675 mL	0.6688 mL
	50 mM	0.0214 mL	0.1070 mL	0.2140 mL	0.5350 mL
	60 mM	0.0178 mL	0.0892 mL	0.1783 mL	0.4459 mL

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Keywords

Gefitinib-based PROTAC 3

4 Cited Publications

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Gefitinib-based PROTAC 3

Publications Citing Use of MedChemExpress (MCE) Gefitinib-based PROTAC 3

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen