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EGFR/HER2-IN-6

EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC₅₀s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 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.: 2820126-50-7
Formula: C₁₈H₂₁N₅O₃S
Molecular Weight:387.46

Storage:

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

Data Sheet (278 KB)

EGFR/HER2-IN-6 Chemical Structure

CAS No.: 2820126-50-7

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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
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 0.122 μM (EGFR kinase), 0.078 μM (HER2 kinase), 0.585 μM (DHFR)^[1]

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	16.18 μM Compound: 43	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	9.43 μM Compound: 43	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	12.18 μM Compound: 43	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	2.37 μM Compound: 43	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	18.39 μM Compound: 43	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	36.84 μM Compound: 43	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-6 (0-100 μM; 72 h) shows remarkable broad spectrum cytotoxic potency, and the cytotoxic potency against MCF7 cells is more potent than SOR^[1].
EGFR/HER2-IN-6 (0-20 μM; 0-48 h) affects cell cycle and indeces apoptosis of MCF-7 cells^[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, MCF7 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:

Exhibited cytotoxic potency to HepG2, MCF7, HCT-116, PC-3 and Hela cell lines with IC₅₀s of 12.18, 2.37, 16.18, 18.39 and 9.43 μM. Showed a lower cytotoxic potency to WI-38 normal cell line with an IC₅₀ value of 36.84 μM.

Apoptosis Analysis^[1]

Cell Line:

MCF-7 breast cancer cell line
Concentration:

0-20 μM
Incubation Time:

0-48 hours
Result:

Through arrested cell cycle at G1/S and G1 phases and induced apoptosis in MCF-7 cells rather than necrosis to achieve anti-breast cancer activity.

In Vivo

EGFR/HER2-IN-6 (10 mg/kg; i.p. once per day for 20days) shows anti-breast cancer activity in mice^[1].

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

Animal Model:

8-week-old swiss albino female mice^[1]
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection; 10 mg/kg once per day; for 20 days
Result:

Decreased tumor volume 65.3% and reduced body weight 7.4% after 20 days of treatment.

Chemical Information

CAS No. 2820126-50-7
Molecular Weight 387.46
Formula C₁₈H₂₁N₅O₃S
SMILES

O=C(C1=CSC2=NC(CN3CCOCC3)=C(C4=CC=C(OC)C=C4)N21)NN
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 (278 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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