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Cat. No.: HY-170438

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EGFR-IN-139

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.

CAS No.: 1574321-31-5
Formula: C₂₇H₂₅ClN₂O₄
Molecular Weight:476.95

Storage:

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

Data Sheet (270 KB)

EGFR-IN-139 Chemical Structure

CAS No.: 1574321-31-5

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Use of MCE Products

Antibody-Drug Conjugates

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

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All EGFR Isoforms :

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).

Chemical Information

CAS No. 1574321-31-5
Molecular Weight 476.95
Formula C₂₇H₂₅ClN₂O₄
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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]. 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]

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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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