Cat. No.: HY-175252

PROTAC EGFR degrader 14

Name: PROTAC EGFR degrader 14
Brand: MedChemExpress
SKU: HY-175252
Price: 420.00 USD
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PROTAC EGFR degrader 14 is a EGFR PROTAC degrader, with a DC₅₀ of 2.9 nM against EGFR^{L858R/T790M/C797S}. PROTAC EGFR degrader 14 forms a stable ternary complex by bridging the ATP-binding pocket of the target protein EGFR with VHL E3 ubiquitin ligase, induces efficient and specific degradation of EGFR mutants via the ubiquitin-proteasome system, and ultimately induces cell cycle arrest and apoptosis. PROTAC EGFR degrader 14 can be used in studies related to non-small cell lung cancer carrying the EGFR^C797S drug-resistant mutation.
(Pink: EGFR ligand (HY-143337); Blue: VHL ligand (HY-125845); Black: linker (HY-W004688)).

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Pureté: 99.26%
Formule: C₅₇H₇₃N₁₁O₄S
Masse moléculaire:1008.33

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PROTAC EGFR degrader 14 Chemical Structure

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

PROTAC EGFR degrader 14 is a EGFR PROTAC degrader, with a DC₅₀ of 2.9 nM against EGFR^{L858R/T790M/C797S}. PROTAC EGFR degrader 14 forms a stable ternary complex by bridging the ATP-binding pocket of the target protein EGFR with VHL E3 ubiquitin ligase, induces efficient and specific degradation of EGFR mutants via the ubiquitin-proteasome system, and ultimately induces cell cycle arrest and apoptosis. PROTAC EGFR degrader 14 can be used in studies related to non-small cell lung cancer carrying the EGFR^C797S drug-resistant mutation^[1]. (Pink: EGFR ligand (HY-143337); Blue: VHL ligand (HY-125845); Black: linker (HY-W004688)).

IC₅₀ & Target

^[1]

EGFR^{L858R/T790M/C797S}

2.9 nM (DC₅₀)

ERK

Bax

Bcl-2

p-STAT3

Voir tous les produits spécifiques à Isoform PROTACs :

Voir tous les produits spécifiques à Isoform EGFR :

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Cellular Effect

Cell Line	Type	Value	Description	References
PC-9	IC₅₀	26.8 nM	Antiproliferative activity against human NSCLC PC9 (EGFR^{L858R/T790M/C797S}) cells assessed as reduction in cell viability incubated for 3 days by CCK-8 assay. Antiproliferative activity against human NSCLC PC9 (EGFR^{L858R/T790M/C797S}) cells assessed as reduction in cell viability incubated for 3 days by CCK-8 assay.	40640988
PC-9	IC₅₀	25.9 nM	Antiproliferative activity against human NSCLC PC9 (EGFR^{L858R/T790M/C797S}) cells assessed as reduction in cell viability incubated for 7 days by CCK-8 assay. Antiproliferative activity against human NSCLC PC9 (EGFR^{L858R/T790M/C797S}) cells assessed as reduction in cell viability incubated for 7 days by CCK-8 assay.	40640988
GES1	IC₅₀	>10 μM	Cytotoxicity against human gastric epithelial GES-1 cells assessed as reduction in cell viability incubated for 72 h by CCK-8 assay. Cytotoxicity against human gastric epithelial GES-1 cells assessed as reduction in cell viability incubated for 72 h by CCK-8 assay.	40640988
BEAS-2B	IC₅₀	>10 μM	Cytotoxicity against human normal lung epithelial BEAS-2B cells assessed as reduction in cell viability incubated for 72 h by CCK-8 assay. Cytotoxicity against human normal lung epithelial BEAS-2B cells assessed as reduction in cell viability incubated for 72 h by CCK-8 assay.	40640988

In Vitro

PROTAC EGFR degrader 14 (Compound 9ea) (4 nM-20 μM; 24 h) efficiently and selectively degrades EGFR^{L858R/T790M/C797S} in PC9 (EGFR^{L858R/T790M/C797S}) cells in a concentration-dependent manner, with a DC₅₀ of 2.9 nM, whereas it shows no obvious degradation activity in A549 (EGFR^WT) cells^[1].
PROTAC EGFR degrader 14 (0.25 μM; 4-24 h) reduces EGFR fluorescence intensity in a time-dependent manner in PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/L858R/C797S}) cells^[1].
PROTAC EGFR degrader 14 (3-7 days) potently inhibits cell proliferation in PC9 (EGFR^{L858R/T790M/C797S}) cells, with an IC₅₀ of 26.8 nM (3 days)/25.9 nM (7 days); it exhibits extremely low cytotoxicity in normal human lung epithelial cells (BEAS-2B) and gastric epithelial cells (GES-1) (IC₅₀ > 10 μM)^[1].
PROTAC EGFR degrader 14 (0.1-5 μM; 24 h) dose-dependently induces G1/G0 cell cycle arrest, reduces S-phase cell population, concentration-dependently promotes early and late cell apoptosis, effectively inhibits EGFR and its downstream signaling pathways, and regulates apoptosis-related proteins in PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/T790M/C797S}) cells, but exerts weak inhibitory effects in A549 (EGFR^WT) cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

PC9 (EGFR^{L858R/T790M/C797S}), PC9 (^{EGFRDel19/T790M/C797S}), and A549 (EGFR^WT) cells
Concentration:

0.25 nM, 0.5 nM, 1 nM, 2 nM, 4 nM, 8 nM, 16 nM, 32 nM, 63 nM, 125 nM, 250 nM, 500 nM, 5 μM, 10 μM, 20 μM
Incubation Time:

24 h
Result:

Potently and dose-dependently degraded EGFR proteins harboring the C797S mutation (DC₅₀ = 2.9 nM for the L858R mutant, DC₅₀ = 21.6 nM for the Del19 mutant), while showing extremely weak degradation of wild-type EGFR (A549 cells), indicating high selectivity.

Immunofluorescence^[1]

Cell Line:

PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/L858R/C797S}) cells
Concentration:

0.25 μM
Incubation Time:

4, 12, 24 h
Result:

Induced the degradation of mutant EGFR proteins in a time-dependent manner, significantly weakening the fluorescence signal.

Cell Cycle Analysis^[1]

Cell Line:

PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/L858R/C797S}) cells
Concentration:

0.1, 0.5, 1, 5 μM
Incubation Time:

24 h
Result:

Arrested the cell cycle at the G1/G0 phase in a dose-dependent manner and significantly reduced the proportion of cells in the S phase.

Apoptosis Analysis^[1]

Cell Line:

PC9 (EGFR^{L858R/T790M/C797S}) and PC9 (EGFR^{Del19/L858R/C797S}) cells
Concentration:

0.1, 0.5, 1, 5 μM
Incubation Time:

48 h
Result:

Significantly promoted early and late apoptosis of resistant NSCLC cells in a concentration-dependent manner, outperforming osimertinib at the same concentrations.

Western Blot Analysis^[2]

Cell Line:

PC9 (^{EGFRL858R/T790M/C797S}), PC9 (EGFR^{Del19/L858R/C797S}), and A549 (EGFR^WT) cells
Concentration:

0.01, 0.05, 0.25 μM
Incubation Time:

24 h
Result:

Effectively inhibited the activation of downstream EGFR signaling pathways (p-EGFR, p-AKT, p-Erk, p-STAT3) in mutant cells, upregulated the pro-apoptotic protein Bax, and downregulated the anti-apoptotic protein Bcl-2.

In Vivo

PROTAC EGFR degrader 14 (Compound 9ea) (25-50 mg/kg; i.v.; once every other day; 16 days) significantly inhibits tumor growth and effectively eliminates EGFR protein in tumor tissues in PC9 (EGFR^{L858R/T790M/C797S}) xenograft mouse models^[1].
PROTAC EGFR degrader 14 (25-50 mg/kg; i.v.; once every other day; 2 weeks) exhibits favorable safety in healthy BALB/c mice, causing no significant body weight loss, no toxic damage to major organs including the heart, liver, spleen, lung, kidney and brain, and no adverse effects on hematological parameters and blood biochemical parameters^[1].

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

Animal Model:

BALB/c nude (male, 6-8 weeks old) were subcutaneously injected with PC9 (EGFR^{L858R/T790M/C797S}) cells^[1]
Dosage:

25 mg/kg, 50 mg/kg
Administration:

i.v.; once every other day; 16 days
Result:

Achieved a 74.7% tumor growth inhibition (TGI) rate at 50 mg/kg, superior to the TGI rate of osimertinib at the same dose.
Significantly reduced average tumor weight compared to vehicle and osimertinib-treated groups at both doses.
Reduced EGFR protein levels in tumor tissues to 0.32 (25 mg/kg) and 0.35 (50 mg/kg) relative to vehicle.
Caused no significant body weight loss during treatment.

Animal Model:

BALB/c nude (male, 6-8 weeks old)^[1]
Dosage:

25 mg/kg, 50 mg/kg
Administration:

i.v.; once every other day; 2 weeks
Result:

Caused no significant weight loss or abnormal behavior in mice, and no EGFR TKI-associated dose-limiting toxicities were observed.
Displayed no obvious toxicity to primary organs, including the heart, liver, spleen, lungs, kidneys, and brain.
Had no toxicity to the circulatory system and normal tissues and possessed a favorable safety profile.

Chemical Information

Appearance Solid
Masse moléculaire 1008.33
Formule C₅₇H₇₃N₁₁O₄S
Color White to light yellow
SMILES

O=C(CCCCCCN1CCN(C2=CC=C(NC3=NC=C4C(N(C(CNC5=CC=CC=C5)=C4)C6CCCC6)=N3)C=C2)CC1)N[C@@H](C(C)(C)C)C(N7[C@H](C(NCC8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (99.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

0.9917 mL

4.9587 mL

9.9174 mL

5 mM

0.1983 mL

0.9917 mL

1.9835 mL

10 mM

0.0992 mL

0.4959 mL

0.9917 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (288 KB)
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)
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)
Instruction de manipulation (2659 KB)

Références

[1]. Wang X, et al. Discovery of a Novel EGFR PROTAC Degrader against C797S Resistance Mutation with Potent Antitumor Efficacy in NSCLC Treatment. Journal of medicinal chemistry. 2025 Jul 24;68(14):14569-14593. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	0.9917 mL	4.9587 mL	9.9174 mL	24.7935 mL
	5 mM	0.1983 mL	0.9917 mL	1.9835 mL	4.9587 mL
	10 mM	0.0992 mL	0.4959 mL	0.9917 mL	2.4793 mL
	15 mM	0.0661 mL	0.3306 mL	0.6612 mL	1.6529 mL
	20 mM	0.0496 mL	0.2479 mL	0.4959 mL	1.2397 mL
	25 mM	0.0397 mL	0.1983 mL	0.3967 mL	0.9917 mL
	30 mM	0.0331 mL	0.1653 mL	0.3306 mL	0.8264 mL
	40 mM	0.0248 mL	0.1240 mL	0.2479 mL	0.6198 mL
	50 mM	0.0198 mL	0.0992 mL	0.1983 mL	0.4959 mL
	60 mM	0.0165 mL	0.0826 mL	0.1653 mL	0.4132 mL
	80 mM	0.0124 mL	0.0620 mL	0.1240 mL	0.3099 mL

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PROTAC EGFR degrader 14

Voir tous les produits spécifiques à Isoform PROTACs

Voir tous les produits spécifiques à Isoform EGFR

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform ERK

Voir tous les produits spécifiques à Isoform STAT

Voir tous les produits spécifiques à Isoform Bcl-2 Family