EGFR-IN-139

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Data Sheet Handling Instructions Technical Support

EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC₅₀s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research_[1].

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

EGFR-IN-139 Chemical Structure

CAS No. : 1574321-31-5

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

EGFR-IN-139 (1 μM, 2 h) inhibits wild-type EGFR and L858R/T790M EGFR with inhibition rates of 90-100% and 65-75% , respectively^[1].
EGFR-IN-139 (0-100 μM, 72 h) inhibits A549, H1975, Vero cells with IC₅₀ s of 28.23 , 29.46, 180.9 μM, respectively^[1].

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

Cell Proliferation Assay

Cell Line:	A549, H1975 cells
Concentration:	0-100 μM
Incubation Time:	72 h
Result:	Inhibited A549, H1975, Vero cells with IC₅₀s of 28.23 (similar to that of Erlotinib (HY-50896)), 29.46, 180.9 μM,. Was relatively safe for normal cells, as its IC₅₀ value in Vero cells was higher compared to those in A549 (SI(IC₅₀ of A549 and H1975) versus IC₅₀ of Vero) of 6.40) and H1975 (SI of 6.14).

Molecular Weight

476.95

Formula

C₂₇H₂₅ClN₂O₄

CAS No.

1574321-31-5

SMILES

O=C(C1=CC=C2OCCOC2=C1)C(O3)=CC4=C3C(C)=NC=C4CN5CC6=C(C=CC=C6)CC5.Cl

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]. Todsaporn D, et al. Furopyridine Derivatives as Potent Inhibitors of the Wild Type, L858R/T790M, and L858R/T790M/C797S EGFR. J Phys Chem B. 2024 Dec 19;128(50):12389-12402. [Content Brief]

EGFR-IN-139 Related Classifications

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The dilution calculator equation

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR-IN-1391574321-31-5EGFREpidermal growth factor receptorErbB-1HER1nonsmall cell lung cancer (NSCLC)drug-sensitiveanticancerInhibitorinhibitorinhibit

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