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Cat. No.: HY-163396

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EGFR-IN-107

EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC₅₀ values of 0.4333 μM for EGFR^WT and 0.0438 μM for EGFR^L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research.

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

Formula: C₃₄H₃₆FN₇O₂
Molecular Weight:593.69

Storage:

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

Data Sheet (275 KB)

EGFR-IN-107 Chemical Structure

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Top Publications Citing

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

Biological Activity

Description

All EGFR Isoforms :

In Vitro

EGFR-IN-107 (compound 3r) has an IC₅₀ value of 5 nM for EGFR kinase^[1].
EGFR-IN-107 has an IC₅₀ value of 1.9 μM against the Osimertinib (HY-15772 ) -resistant H1975 cell line (H1975OR)^[1].
EGFR-IN-107 (1 μM, 24 h) induces apoptosis and inhibits cell migration in H1975 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

H1975 cells
Concentration:

1 μM
Incubation Time:

24h
Result:

Up-regulated the expression levels of Bax, cleaved caspase-3 and E-cadherin, and down-regulated the expression levels of matrix metalloproteinase-2 (MMP-2) and anti-apoptotic marker Bcl-2.

In Vivo

EGFR-IN-107 (compound 3r) (5, 10, 20 mg/kg; Oral gavage (p.o.); 21 days) has strong antitumor activity in H1975 xenografted mouse models and can significantly inhibit the proliferation of H1975 xenografted mouse models^[1].

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

Animal Model:

H1975 xenograft mouse model^[1]
Dosage:

5, 10, 20 mg/kg
Administration:

Oral gavage (p.o.); 21days
Result:

At 20 mg/kg showed the same antitumor effect as Osimertinib (HY-15772) (20 mg/kg).
Leaded to the down-regulation of p-EGFR.
Did not cause significant weight loss or tissue damage.

Chemical Information

Molecular Weight 593.69
Formula C₃₄H₃₆FN₇O₂
SMILES

C=CC(NC1=C(C=C(C(NC2=NC(C3=C(N(C4=C3C=CC=C4)C)C5=CC=CC(F)=C5)=CC=N2)=C1)OC)N(CCN(C)C)C)=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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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]. Feng R, et al. Late-stage modification of complex drug: Base-controlled Pd-catalyzed regioselective synthesis and bioactivity of arylated osimertinibs. Sci Adv. 2024 Mar 8;10(10):eadl0026. [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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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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EGFR-IN-107

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-107 Related Classifications

HY-163396 Related Classifications