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Cat. No.: HY-187534

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VEGFR2 AUTOTAC-1

VEGFR2 AUTOTAC-1 is a VEGFR2 AUTOTAC degrader. VEGFR2 AUTOTAC-1 recruits p62, activates the autophagy-lysosome pathway through the p62-LC3 axis cascade, forms a ternary complex with VEGFR2 and p62, and drives UPS-independent post-translational degradation of VEGFR2. VEGFR2 AUTOTAC-1 induces G1 phase arrest and endogenous apoptosis in cells via the mitochondrial and caspase apoptotic pathways, thereby inhibiting cancer cell proliferation, migration and malignant phenotypes; meanwhile, it inhibits endothelial cell tube formation, migration and endothelial-mesenchymal transition by regulating E-cadherin and MMP2. VEGFR2 AUTOTAC-1 is applicable to research related to triple-negative breast cancer.(Pink: VEGFR2 target protein ligand (HY-187558); Blue: p62 ligand (HY-W014292); Black: Linker)

For research use only. We do not sell to patients.

Formula: C₄₆H₅₆N₈O₂
Molecular Weight:752.99

Storage:

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

VEGFR2 AUTOTAC-1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

VEGFR2

MMP2

E-cadherin (CDH1)

All VEGFR Isoforms :

All MMP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-468	IC50	0.74 μM	Antiproliferative activity against human MDA-MB-468 cells assessed via viability assay. Antiproliferative activity against human MDA-MB-468 cells assessed via viability assay.	42481435

In Vitro

Anti-cancerAutophagyApoptosisCell Cycle RegulationOthers

Anti-cancer

Autophagy

VEGFR2 AUTOTAC-1 (Compound 11bg) (2.5 μM; 24 h) significantly activates autophagy in MDA-MB-231, MDA-MB-468 and MDA-MB-436 cells^[1].
VEGFR2 AUTOTAC-1 (1-2.5 μM; 12-48 h) promotes the accumulation of p62 and LC3-II in MDA-MB-468 cells^[1].

Anti-cancer

Apoptosis

Cell Cycle Regulation

VEGFR2 AUTOTAC-1 (0.5-5 μM; 48 h) concentration-dependently inhibits colony formation, induces G1-phase cell cycle arrest and apoptosis, upregulates pro-apoptotic proteins and downregulates anti-apoptotic proteins, and suppresses cell migration in MDA-MB-468 cells^[1].

Others

VEGFR2 AUTOTAC-1 (2.5 μM; 3 min) increases the thermal stability of VEGFR2 and p62 proteins in MDA-MB-468 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231, MDA-MB-468, MDA-MB-436
Concentration:

2.5 μM
Incubation Time:

24 h
Result:

Significantly activated intracellular autophagy.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-468
Concentration:

0.5, 1, 1.5, 2.5, 5 μM
Incubation Time:

8, 16, 24, 48 h
Result:

Decreased VEGFR2 protein levels in a concentration- and time-dependent manner.

Real Time qPCR^[1]

Cell Line:

MDA-MB-468
Concentration:

0.5, 1, 1.5, 2.5, 5 μM
Incubation Time:

8, 16, 24, 48 h
Result:

Did not significantly alter VEGFR2 mRNA expression levels.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-468
Concentration:

1, 1.5, 2.5 μM
Incubation Time:

12, 24, 48 h
Result:

Induced the accumulation of p62 and LC3-II.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-468
Concentration:

0.5, 1, 2.5 μM
Incubation Time:

48 h
Result:

Induced cell cycle arrest at the G1 phase.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-468
Concentration:

0.5, 1, 2.5 μM
Incubation Time:

48 h
Result:

Induced cell apoptosis.

Cell Proliferation Assay^[1]

Cell Line:

HUVEC
Concentration:

2.5, 5 μM
Incubation Time:

6, 12, 24 h
Result:

Significantly inhibited VEGF165-induced endothelial cell tube formation.

Western Blot Analysis^[1]

Cell Line:

HUVEC
Concentration:

1, 2.5, 5 μM
Incubation Time:

24 h
Result:

Upregulated E-cadherin and downregulated MMP-2.

Related Protocols :

Chemical Information

Molecular Weight 752.99
Formula C₄₆H₅₆N₈O₂
SMILES

CC1=C2C=CC(N(C3=NC(NC4=CC=C(C(C(NCCCCCCCCCCNCC5=CC=CC(OCC6=CC=CC=C6)=C5)=O)=C4)C)=NC=C3)C)=CC2=NN1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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

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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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

Product Name:
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MCE Japan Authorized Agent:

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VEGFR2 AUTOTAC-1

All VEGFR Isoforms

All MMP Isoforms