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Art. -Nr.: HY-187533

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EGFR AUTOTAC-1

EGFR AUTOTAC-1 is a p62/SQSTM1-directed EGFR AUTOTAC degrader. EGFR AUTOTAC-1 recruits p62 to form a ternary complex, activates the ubiquitin-proteasome system-independent Atg5-dependent autophagy-lysosome pathway, mediates autophagic degradation of EGFR and inhibits the AKT/ERK signaling pathway, thereby promoting apoptosis and activating autophagy. EGFR AUTOTAC-1 can be used for the research of non-small cell lung cancer.
(Pink: Autophagy and EGFR ligand (HY-79511); Blue: Ligands for E3 Ligase E3 ligase ligand; Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₂H₃₈ClF₅N₄O₄
Molecular Weight:793.22

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

EGFR AUTOTAC-1 Chemical Structure

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

EGFR AUTOTAC-1 is a p62/SQSTM1-directed EGFR AUTOTAC degrader. EGFR AUTOTAC-1 recruits p62 to form a ternary complex, activates the ubiquitin-proteasome system-independent Atg5-dependent autophagy-lysosome pathway, mediates autophagic degradation of EGFR and inhibits the AKT/ERK signaling pathway, thereby promoting apoptosis and activating autophagy. EGFR AUTOTAC-1 can be used for the research of non-small cell lung cancer^[1]. (Pink: Autophagy and EGFR ligand (HY-79511); Blue: Ligands for E3 Ligase E3 ligase ligand; Black: linker).

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Cellular Effect

Cell Line	Type	Value	Description	References
HCC827	IC50	6.65 μM	Antiproliferative activity against human HCC827 cells assessed as reduction in cell proliferation incubated for 24 hrs by CCK-8 assay. Antiproliferative activity against human HCC827 cells assessed as reduction in cell proliferation incubated for 24 hrs by CCK-8 assay.	42481435
HCC827	IC50	4.75 μM	Antiproliferative activity against human HCC827 cells assessed as reduction in cell proliferation incubated for 48 hrs by CCK-8 assay. Antiproliferative activity against human HCC827 cells assessed as reduction in cell proliferation incubated for 48 hrs by CCK-8 assay.	42481435
HCC827	IC50	4.37 μM	Antiproliferative activity against human HCC827 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human HCC827 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	42481435
HCC827	IC50	3.89 μM	Antiproliferative activity against human HCC827 cells assessed as reduction in cell proliferation incubated for 96 hrs by CCK-8 assay. Antiproliferative activity against human HCC827 cells assessed as reduction in cell proliferation incubated for 96 hrs by CCK-8 assay.	42481435

In Vitro

EGFR AUTOTAC-1 (Compound 6d) (0.5-10 μM; 12-24 h) promotes the degradation of EGFR protein in a concentration-dependent and time-dependent manner in HCC827 cells^[1].
EGFR AUTOTAC-1 (0.5-7.5 μM; 4-24 h) does not affect EGFR mRNA transcription levels in HCC827 cells, but promotes the accumulation of p62 and LC3-II in a concentration- and time-dependent manner ^[1].
EGFR AUTOTAC-1 (5.0 μM; 24 h) exerts weak or insignificant EGFR-degrading effects in A549 and H1975 cells, demonstrating conformational selectivity^[1].
EGFR AUTOTAC-1 (5.0 μM; 3 min) enhances the thermal stability of EGFR and p62 proteins in HCC827 cells, confirming its targeted binding ability^[1].
EGFR AUTOTAC-1 (5.0 μM; 24 h) induces the formation and colocalization of p62 and LC3 puncta in HCC827 cells^[1].
EGFR AUTOTAC-1 (0.5-7.5 μM) inhibits cell colony formation and scratch wound healing in HCC827 cells^[1].
EGFR AUTOTAC-1 (1-5 μM; 48 h) induces G0/G1 cell cycle arrest and apoptosis in HCC827 cells^[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:

0.5, 1, 2.5, 5, 7.5, 10 μM
Incubation Time:

4, 8, 12, 24 h
Result:

Decreased EGFR protein levels in a concentration-dependent manner.
Induced EGFR degradation in a time-dependent manner.

Real Time qPCR^[1]

Cell Line:

HCC827 cells
Concentration:

0.5, 1, 2.5, 5, 7.5 μM and 5.0 μM
Incubation Time:

4, 8, 12, 24 h
Result:

Did not alter the mRNA expression levels of EGFR.

Immunofluorescence^[1]

Cell Line:

HCC827 cells
Concentration:

5.0 μM
Incubation Time:

24 h
Result:

Induced the formation and colocalization of p62 and LC3 punctate structures.

Cell Cycle Analysis^[1]

Cell Line:

HCC827 cells
Concentration:

1, 2.5, 5 μM
Incubation Time:

48 h
Result:

Significantly induced cell cycle arrest at the G0/G1 phase.

Apoptosis Analysis^[1]

Cell Line:

HCC827 cells
Concentration:

1, 2.5, 5 μM
Incubation Time:

48 h
Result:

Induced cell apoptosis in a concentration-dependent manner.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	T_max	AUC_0-t	AUC_0-∞	V_z	CL	Bioavailability
Rat^[1]	1 mg/kg	i.v.	25.21 h	337.22 μg/L	0.08 h	580.10 μg/L·h	1036.48 μg/L·h	329.91 L/kg	10.43 L/h/kg	/
Rat^[1]	10 mg/kg	p.o.	17.69 h	47.14 μg/L	6.00 h	544.03 μg/L·h	921.23 μg/L·h	252.86 L/kg	11.22 L/h/kg	9.38 %

In Vivo

EGFR AUTOTAC-1 (compound 6d) (5-20 mg/kg; i.p.; multiple administrations; 22 days) dose-dependently inhibits tumor growth, reduces tumor volume and weight, and causes no obvious systemic toxicity in HCC827 xenograft nude mouse models^[1].

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

Animal Model:

Nude mice were injected subcutaneously HCC827 cells to establish the xenograft tumor model^[1]
Dosage:

5 mg/kg, 10 mg/kg, 20 mg/kg
Administration:

i.p.; multiple administrations; 22 days
Result:

Reduced tumor volume and tumor weight in a dose-dependent manner.
Animal body weight remained stable throughout the treatment period, and no significant histopathological changes were observed in major organs (heart, liver, spleen, lung, kidney, and intestine).
Significantly reduced the expression levels of the proliferation marker Ki-67 and the target protein EGFR in tumor tissue sections.
Significantly altered the expression levels of autophagy-related proteins p62 and LC3 in tumor tissues.

Chemical Information

Molecular Weight 793.22
Formel C₄₂H₃₈ClF₅N₄O₄
SMILES

FC1=CC=C(NC2=C3C(C=C(C(OCCCCCCNCC4=CC=C(C(OCC5=CC=C(C(F)=C5)F)=C4)OCC6=CC(F)=C(C=C6)F)=C3)OC)=NC=N2)C=C1Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wu D, et al. Structure-Guided Optimization of p62-Directed AUTOTACs for Efficient EGFR/VEGFR2 Degradation and Antitumor Efficacy. Journal of medicinal chemistry. 2026 Jul 21.

Calculators

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)}

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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EGFR AUTOTAC-1

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