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Cat. No.: HY-189734

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EGFR/VEGFR2-IN-14

EGFR/VEGFR2-IN-14 is an EGFR/VEGFR2 kinase inhibitor (EGFR^WT IC₅₀ 0.068 μM, EGFR^T790M IC₅₀ 0.154 μM, VEGFR-2 IC₅₀ 0.071 μM). EGFR/VEGFR2-IN-14 is associated with G0/G1 phase arrest. EGFR/VEGFR2-IN-14 exhibits anticancer activity against lung cancer, breast cancer, and colorectal cancer. EGFR/VEGFR2-IN-14 can be used for cancer research.

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

Formula: C₂₅H₁₇ClN₆O₂S
Molecular Weight:500.96

Storage:

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

EGFR/VEGFR2-IN-14 Chemical Structure

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

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

0.071 μM (IC₅₀)

EGFR (WT)

0.068 μM (IC₅₀)

EGFR^T790M

0.154 μM (IC₅₀)

All EGFR Isoforms :

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC50	5.43 μM	Antiproliferative activity against human A549 cells assessed as viability reduction after 48 hrs by MTT assay. Antiproliferative activity against human A549 cells assessed as viability reduction after 48 hrs by MTT assay.	42715623
MCF7	IC50	4.6 μM	Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction after 48 hrs by MTT assay. Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction after 48 hrs by MTT assay.	42715623
HCT-116	IC50	12.62 μM	Antiproliferative activity against human HCT-116 colon cancer cells assessed as viability reduction after 48 hrs by MTT assay. Antiproliferative activity against human HCT-116 colon cancer cells assessed as viability reduction after 48 hrs by MTT assay.	42715623
FHC	IC50	72.56 μM	Cytotoxicity against fetal human colon normal epithelial FHC cells assessed as viability reduction after 48 hrs by MTT assay. Cytotoxicity against fetal human colon normal epithelial FHC cells assessed as viability reduction after 48 hrs by MTT assay.	42715623
NCI-H1975	IC50	16.794 μM	Cytotoxicity against human NCI-H1975 EGFR T790M mutant NSCLC cells assessed as viability reduction after 48 hrs by MTT assay. Cytotoxicity against human NCI-H1975 EGFR T790M mutant NSCLC cells assessed as viability reduction after 48 hrs by MTT assay.	42715623
SW1463	IC50	7.180 μM	Cytotoxicity against human SW1463 KRAS-mutant colorectal carcinoma cells assessed as viability reduction after 48 hrs by MTT assay. Cytotoxicity against human SW1463 KRAS-mutant colorectal carcinoma cells assessed as viability reduction after 48 hrs by MTT assay.	42715623

In Vitro

Anti-cancerCell Cycle RegulationOthers

Anti-cancer

EGFR/VEGFR2-IN-14 (Compound 8d) (0.4-100 μM; 48 h) exhibited MTT IC₅₀ values of 5.43 μM in A549 cells, 4.6 μM in MCF-7 cells, 12.62 μM in HCT-116 cells, and 72.56 μM in FHC cells^[1].
EGFR/VEGFR2-IN-14 (24 h) reduced EGFR^T790M expression to 2.164 ng/mL in NCI-H1975 cells and EGFR^WT expression to 220.88 pg/mL in SW1463 cells in a cell-based ELISA^[1].

Anti-cancer

Cell Cycle Regulation

EGFR/VEGFR2-IN-14 (12.62 μM; 48 h) altered cell cycle distribution in HCT-116 cells, with an increase in the G0/G1 phase and decreases in the S and G2/M phases, and it was subsequently reported to cause S phase accumulation^[1].

Others

EGFR/VEGFR2-IN-14 (0.01-100 μM; EGFR 40 min, VEGFR-2 45 min) inhibits EGFR^WT (IC₅₀ 0.068 μM), EGFR^T790M (IC₅₀ 0.154 μM), and VEGFR-2 (IC₅₀ 0.071 μM) in cell-free kinase assays^[1].

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

Cell Viability Assay^[1]

Cell Line:

A549, MCF-7, HCT-116, and FHC cells
Concentration:

100, 25, 6.3, 1.6, 0.4 μM
Incubation Time:

48 h (after 24 h seeding; MTT 2-4 h)
Result:

IC₅₀ values were 5.43 μM in A549, 4.6 μM in MCF-7, 12.62 μM in HCT-116, and 72.56 μM in FHC cells.
In the HCT-116/FHC model, the relative cytotoxicity ratio was 5.75.

Cell Cycle Analysis^[1]

Cell Line:

HCT-116 cells
Concentration:

12.62 μM
Incubation Time:

48 h; PI staining 30 min at 37 °C
Result:

An increase in the G0/G1 population occurred, accompanied by a decrease in S and G2/M phases.
A later comparison reported notable accumulation of cells in the S phase.

Related Protocols :

Chemical Information

Molecular Weight 500.96
Formula C₂₅H₁₇ClN₆O₂S
SMILES

O=C(/C=C/C1=CC=C(Cl)C=C1)C2=CC=C(N3C=C(CSC4=NN=C(C5=CC=NC=C5)O4)N=N3)C=C2
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]. El-Qommos M, et al. New oxa/thiadiazole-chalcone hybrids linked via a clickable 1,2,3-triazole bridge with dual EGFR/VEGFR-2 kinase inhibitory activity and antiproliferative effects. Bioorganic chemistry. 2026 Aug 31;182:110453.

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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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100 mg

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

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EGFR/VEGFR2-IN-14

All EGFR Isoforms

All VEGFR Isoforms