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Cat. No.: HY-161785

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EGFR-IN-117

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR^{L858R/T790M/C797S} and BaF3–^{C797S/Del19/T790M}, with IC₅₀ of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models.

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

CAS No.: 3035639-05-2
Formula: C₂₅H₃₀BrN₇O₂S
Molecular Weight:572.52

Storage:

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

Data Sheet (271 KB)

EGFR-IN-117 Chemical Structure

CAS No.: 3035639-05-2

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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
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
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Bioz

Biological Activity

Description

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.003 nM Compound: 8h	Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/Del19/T790M mutant Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/Del19/T790M mutant	[PMID: 38908104]
BaF3	IC₅₀	0.004 nM Compound: 8h	Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/L858R/T790M mutant Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/L858R/T790M mutant	[PMID: 38908104]
BaF3	IC₅₀	11.15 nM Compound: 8h	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as inhibition of sphere formation incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as inhibition of sphere formation incubated for 72 hrs by CCK8 assay	[PMID: 38908104]
HaCaT	IC₅₀	5.414 μM Compound: 8h	Cytotoxicity against human HaCaT cells Cytotoxicity against human HaCaT cells	[PMID: 38908104]
HK-2	IC₅₀	2.785 μM Compound: 8h	Cytotoxicity against human HK-2 cells Cytotoxicity against human HK-2 cells	[PMID: 38908104]
HUVEC	IC₅₀	0.799 μM Compound: 8h	Cytotoxicity against VEGF-stimulated human HUVEC cells Cytotoxicity against VEGF-stimulated human HUVEC cells	[PMID: 38908104]
HUVEC	IC₅₀	2.515 μM Compound: 8h	Cytotoxicity against human HUVEC cells Cytotoxicity against human HUVEC cells	[PMID: 38908104]
L02	IC₅₀	4.354 μM Compound: 8h	Cytotoxicity against human L02 cells Cytotoxicity against human L02 cells	[PMID: 38908104]
NCI-H1975	IC₅₀	0.013 nM Compound: 8h	Antiproliferative activity against human NCI-H1975 cells harboring EGFR double mutation Antiproliferative activity against human NCI-H1975 cells harboring EGFR double mutation	[PMID: 38908104]
NCI-H1975	IC₅₀	33.83 nM Compound: 8h	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of sphere formation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of sphere formation incubated for 72 hrs by CCK8 assay	[PMID: 38908104]
PC-9	IC₅₀	0.019 nM Compound: 8h	Antiproliferative activity against human PC-9 cells harboring EGFR single mutation Antiproliferative activity against human PC-9 cells harboring EGFR single mutation	[PMID: 38908104]

Chemical Information

CAS No. 3035639-05-2
Molecular Weight 572.52
Formula C₂₅H₃₀BrN₇O₂S
SMILES

O=S(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCCN(C)CC4)C=C3)=NC=C2Br)(C5CC5)=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 (271 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]. Yao H, et al., Discovery of new cyclopropane sulfonamide derivatives as EGFR inhibitors to overcome C797S-mediated resistance and EGFR double mutation. Eur J Med Chem. 2024 Jun 16;275:116590. [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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