1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. EGFR-IN-74

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

EGFR-IN-74 Chemical Structure

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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]

EGFRL858R/T790M

138 nM (IC50)

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

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
References
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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.

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Product Name:
EGFR-IN-74
Cat. No.:
HY-151981
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