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Cat. No.: HY-151161

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EGFR/HER2-IN-8

EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC₅₀s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.

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

CAS No.: 2820126-32-5
Formula: C₁₆H₁₆N₄O₂S
Molecular Weight:328.39

Storage:

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

Data Sheet (275 KB)

EGFR/HER2-IN-8 Chemical Structure

CAS No.: 2820126-32-5

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

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
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 0.45 μM (EGFR kinase), 0.244 μM (HER2 kinase), 5.669 μM (DHFR)^[1]

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	9.23 μM Compound: 34	Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay	[PMID: 35964425]
HeLa	IC₅₀	13.02 μM Compound: 34	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 35964425]
HepG2	IC₅₀	7.34 μM Compound: 34	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 35964425]
MCF7	IC₅₀	5.19 μM Compound: 34	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 35964425]
PC-3	IC₅₀	18.5 μM Compound: 34	Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay	[PMID: 35964425]
WI-38	IC₅₀	67.23 μM Compound: 34	Antiproliferative activity against human WI-38 cells after 72 hrs by MTT assay Antiproliferative activity against human WI-38 cells after 72 hrs by MTT assay	[PMID: 35964425]

In Vitro

EGFR/HER2-IN-8 (0-100 μM; 72 h) shows highly potent anticancer activity to HepG2, MCF 7, HCT-116, PC-3 and Hela cell lines and exhibits selective cytotoxicity against cancer cell lines rather than normal cell line^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

HepG2 hepatocellular carcinoma, MCF 7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate, Hea cervical epithelioid carcinoma cell lines and WI-38 fetal lung fibroblast cells
Concentration:

0-100 μM
Incubation Time:

72 hours
Result:

Exibited more potent cytotoxicity than SOR towards HepG2, MCF 7, HCT-116, PC-3 and Hela cell lines with IC₅₀s of 7.34, 5.19, 9.23, 18.5 and 13.02 μM, respectively. Showed weak cytotoxic activity against WI-38 cell line with an IC₅₀ value of 67.25 μM, and possessed best selectivity indices towards MCF-7 breast cancer cell line.

Chemical Information

CAS No. 2820126-32-5
Molecular Weight 328.39
Formula C₁₆H₁₆N₄O₂S
SMILES

O=C(C1=CSC2=NC=C(C3=CC=C(C)C=C3)N21)NNC(CC)=O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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)
Handling Instructions (2659 KB)

References

[1]. Sabry MA, et al. New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity. Eur J Med Chem. 2022 Aug 10;241:114661. [Content Brief]

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.

Keywords

100 mg

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