EGFR-IN-74

Cat. No.: HY-151981: Data Sheet Handling Instructions
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EGFR-IN-74 (Compound 21) is a potent EGFR inhibitor with an IC₅₀ of 138 nM against EGFR L858R/T790M. EGFR-IN-74 induces cancer cell apoptosis.

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

EGFR-IN-74 Chemical Structure

CAS No. : 3037947-20-6

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Biological Activity
Purity & Documentation
References
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Description

EGFR-IN-74 (Compound 21) is a potent EGFR inhibitor with an IC₅₀ of 138 nM against EGFR L858R/T790M. EGFR-IN-74 induces cancer cell apoptosis^[1].

IC₅₀ & Target^[1]

EGFR^L858R/T790M

138 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.99 μM Compound: 21	Anticancer activity against human A549 cells overexpressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay Anticancer activity against human A549 cells overexpressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]
A549	IC₅₀	2.99 μM Compound: 21	Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]
BEAS-2B	IC₅₀	85.14 μM Compound: 21	Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]
HCC827	IC₅₀	0.01 μM Compound: 21	Anticancer activity against human HCC827 cells harboring EGFR E746_A750 del mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Anticancer activity against human HCC827 cells harboring EGFR E746_A750 del mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]
NCI-H1975	IC₅₀	0.21 μM Compound: 21	Anticancer activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Anticancer activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]

In Vitro

EGFR-IN-74 (Compound 21) (72 h) shows anticancer activity against cells harbouring a different status of the EGFR^[1].
EGFR-IN-74 (0.01 μM; 24 and 48 h) induces apoptosis in cancer cells^[1].
EGFR-IN-74 forms a stable complex with the EGFR enzyme without much structural rearrangement^[1].

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

Cell Viability Assay^[1]

Cell Line:	HCC827 (EGFR Del E746-A750), NCI–H1975 (EGFR L858R/T790 M), A549 (WT EGFR), A549 and BEAS-2B cells
Concentration:
Incubation Time:	72 h
Result:	Inhibited cell viability with IC₅₀s of 0.010 ± 0.02, 0.21 ± 0.99, 0.99 ± 0.11, 2.99 ± 0.21 and 85.14 ± 0.12 μM against HCC827 (EGFR Del E746-A750), NCI–H1975 (EGFR L858R/T790 M), A549 (WT EGFR), A549 and BEAS-2B cells respectively.

Western Blot Analysis^[1]

Cell Line:	HCC827 cells
Concentration:	0.01, 0.10 and 1.00 μM
Incubation Time:
Result:	Showed an ability to phosphorylate AKT.

Apoptosis Analysis^[1]

Cell Line:	HCC827 cells
Concentration:	0.010 μM (IC₅₀ value)
Incubation Time:	24 and 48 h
Result:	Induced early apoptosis and late apoptosis of 26.8% and 4.2% respectively, in comparison with control, with early apoptosis of 2.1% and late apoptosis of 1.1%.

Molecular Weight

729.57

Formula

C₃₂H₂₈BrF₃N₆O₄S

CAS No.

3037947-20-6

SMILES

CCOC(C1=C(C2=CC(Br)=CC=C2N=C1N3C=CN=C3)N4CCN(CC4)C5=C(C=CC=C5)NS(=O)(C6=CC=C(C=C6)C(F)(F)F)=O)=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

Handling Instructions (2659 KB)

References

[1]. Kardile RA, et al. Design, synthesis, and biological evaluation of novel quinoline derivatives as small molecule mutant EGFR inhibitors targeting resistance in NSCLC: In vitro screening and ADME predictions. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114889. [Content Brief]

EGFR-IN-74 Related Classifications

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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-743037947-20-6EGFREpidermal growth factor receptorErbB-1HER1HCC827NCI–H1975A549Inhibitorinhibitorinhibit

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