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Cat. No.: HY-149695

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EGFR-IN-91

EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR^L858R/C797S and EGFR^{exon 19del/C797S}, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants.

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

CAS No.: 3032113-20-2
Formula: C₂₂H₂₅ClFN₅O₃
Molecular Weight:461.92

Storage:

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

Data Sheet (266 KB)

EGFR-IN-91 Chemical Structure

CAS No.: 3032113-20-2

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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
A-431	IC₅₀	83 nM Compound: 9	Antiproliferative activity against human A-431 cells overexpressing wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human A-431 cells overexpressing wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37934858]
AU565	IC₅₀	986 nM Compound: 9	Antiproliferative activity against patient-derived HER2-positive human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against patient-derived HER2-positive human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37934858]
HCC827	IC₅₀	3.1 nM Compound: 9	Antiproliferative activity against human HCC827 cells harboring EGFR del E746_A750 mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human HCC827 cells harboring EGFR del E746_A750 mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37934858]
NCI-H1975	IC₅₀	>10000 nM Compound: 9	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37934858]
NCI-H3255	IC₅₀	7.2 nM Compound: 9	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37934858]
SK-BR-3	IC₅₀	1510 nM Compound: 9	Antiproliferative activity against patient-derived HER2-positive human SK-BR-3 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against patient-derived HER2-positive human SK-BR-3 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37934858]
ZR-75-30	IC₅₀	1632 nM Compound: 9	Antiproliferative activity against patient-derived HER2-positive human ZR-75-30 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against patient-derived HER2-positive human ZR-75-30 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37934858]

Chemical Information

CAS No. 3032113-20-2
Molecular Weight 461.92
Formula C₂₂H₂₅ClFN₅O₃
SMILES

CN1CCN(OCCOC2=C(OC)C=C3N=CN=C(NC4=CC=CC(Cl)=C4F)C3=C2)CC1
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 (266 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]. Hill J et al. Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer[J]. Journal of Medicinal Chemistry, 2023.

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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
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Purity & Documentation
References

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EGFR-IN-91

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-91 Related Classifications

HY-149695 Related Classifications