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Cat. No.: HY-190476

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VEGFR-2-IN-96

VEGFR-2-IN-96 is a selective type II VEGFR-2 inhibitor (IC₅₀ = 56 nM) and exhibits selective antiproliferative activity against cancer cells. VEGFR-2-IN-96 inhibits VEGFR-2 phosphorylation, downregulates VEGF‑A secretion, induces apoptosis and G2/M cell cycle arrest, and inhibits cancer cell migration. VEGFR-2-IN-96 can be used in research related to hepatocellular carcinoma and breast cancer.

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

Formula: C₂₃H₂₇N₅O₄S
Molecular Weight:469.56

Storage:

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

VEGFR-2-IN-96 Chemical Structure

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Amount: USD 0.00

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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

Caspase-3

Caspase-9

Bcl-2

Bax

All VEGFR Isoforms :

All Caspase Isoforms :

All Bcl-2 Family Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC50	5.38 μM	Antiproliferative activity against HepG2 cells assessed as viability reduction incubated 72 hrs by MTT assay. Antiproliferative activity against HepG2 cells assessed as viability reduction incubated 72 hrs by MTT assay.	42887065
MCF7	IC50	5.92 μM	Antiproliferative activity against MCF-7 cells assessed as viability reduction incubated 72 hrs by MTT assay. Antiproliferative activity against MCF-7 cells assessed as viability reduction incubated 72 hrs by MTT assay.	42887065
Vero	IC50	28.00 μM	Cytotoxicity against Vero cells assessed as viability reduction incubated 72 hrs by MTT assay. Cytotoxicity against Vero cells assessed as viability reduction incubated 72 hrs by MTT assay.	42887065

In Vitro

Anti-cancerApoptosisLocal Vascular Regulation

Anti-cancer

VEGFR-2-IN-96 (0.1-300 μM; 72 h) inhibits the proliferation of HepG2 and MCF-7 cells with IC₅₀ values of 5.38 and 5.92 μM, respectively, while showing lower cytotoxicity against normal Vero cells^[1].
VEGFR-2-IN-96 (0.54-2.69 μM; 48 h) reduces the HepG2 wound healing rate^[1].

Anti-cancer

Apoptosis

VEGFR-2-IN-96 (5.38 μM; 48 h) induces G2/M cell cycle arrest and Sub-G1 accumulation in HepG2 cells and induces significant apoptosis; moreover, it activates the intrinsic apoptotic pathway in HepG2 cells by upregulating Bax, caspase-9, and caspase-3 and downregulating Bcl-2^[1].

Local Vascular Regulation

VEGFR-2-IN-96 (compound 10d) inhibits cell-free VEGFR-2 kinase with an IC₅₀ of 0.056 μM; and its inhibitory activity against VEGFR-2 is superior to its inhibitory activity against PDGFR, FGFR, FLT3-ITD, and ABL^[1].
VEGFR-2-IN-96 (0.5-2 μM) dose-dependently reduces p-VEGFR-2 levels and VEGF-A secretion in HepG2 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

HepG2, MCF-7, and Vero cells
Concentration:

300, 100, 30, 10, 3, 1, 0.3, and 0.1 μM
Incubation Time:

72 h
Result:

Inhibited HepG2 and MCF-7 proliferation with IC₅₀ values of 5.38 and 5.92 μM, respectively, while showing lower cytotoxicity toward normal Vero cells (28.00 μM).

Cell Cycle Analysis^[1]

Cell Line:

HepG2 cells
Concentration:

5.38 μM
Incubation Time:

48 h
Result:

Induced G2/M cell-cycle arrest and Sub-G1 accumulation in HepG2 cells.

Apoptosis Analysis^[1]

Cell Line:

HepG2 cells
Concentration:

5.38 μM
Incubation Time:

48 h
Result:

Induced significant apoptosis, with a total apoptosis rate of 53.29%.

Real Time qPCR^[1]

Cell Line:

HepG2 cells
Concentration:

5.38 μM
Incubation Time:

48 h
Result:

Activated the intrinsic apoptotic pathway in HepG2 cells by upregulating Bax, caspase-9, and caspase-3, and downregulating Bcl-2.

Cell Migration Assay ^[1]

Cell Line:

HepG2 cells
Concentration:

0.54, 2.69 μM
Incubation Time:

48 h
Result:

Reduced HepG2 wound closure to 55.14% and 39.99% at sub-cytotoxic concentrations of 0.54 and 2.69 μM, respectively.

Related Protocols :

Chemical Information

Molecular Weight 469.56
Formula C₂₃H₂₇N₅O₄S
SMILES

O=C(NC1=CC=C(OC)C=C1)CN(CC2)CCN2C3=NC=NC4=C3C(C)=C(C(OCC)=O)S4
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]. Saleh AM, et al. Design of 4-(piperazin-1-yl)thieno[2,3-d]pyrimidine derivatives targeting the DFG-out conformation of VEGFR-2: Synthesis, biological evaluations, and molecular modeling approaches. European journal of medicinal chemistry. 2026 Oct 07;321(Pt 2):119401.

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

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MOQ

Minimum order quantity

100 mg

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

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VEGFR-2-IN-96

All VEGFR Isoforms

All Caspase Isoforms

All Bcl-2 Family Isoforms