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Cat. No.: HY-157432

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EGFR-IN-97

EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR^{L858R/T790M/C797S} and Ba/F3-EGFR^{Del19/T790M/C797S} cells, with IC₅₀ values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR^{L858R/T790M/C797S} cells at the concentration of 0.8 μM.

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

CAS No.: 3020681-05-1
Formula: C₃₇H₃₆N₈O₂
Molecular Weight:624.73

Storage:

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

Data Sheet (267 KB)

EGFR-IN-97 Chemical Structure

CAS No.: 3020681-05-1

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

Biological Activity

Description

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	5.14 μM Compound: 6q	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38142512]
BaF3	IC₅₀	0.41 μM Compound: 6q	Antiproliferative activity against mouse BaF3 cells harboring EGFR Del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring EGFR Del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38142512]
BaF3	IC₅₀	0.41 μM Compound: 6q	Antiproliferative activity against mouse BaF3 cells harboring wildtype EGFR assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring wildtype EGFR assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38142512]
BaF3	IC₅₀	0.42 μM Compound: 6q	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38142512]
BEAS-2B	IC₅₀	5.12 μM Compound: 6q	Antiproliferative activity against human BEAS-2B cells assessed as inhibition of cell growth Antiproliferative activity against human BEAS-2B cells assessed as inhibition of cell growth	[PMID: 38142512]
NCI-H1975	IC₅₀	0.82 μM Compound: 6q	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38142512]
NCI-H1975	IC₅₀	2.95 μM Compound: 6q	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38142512]

In Vitro

EGFR-IN-97 (compound 6q) shows excellent activity against mutant NSCLC cell line NCI-H1975-EGFR^{L858R/T790M/C797S} cells, with IC₅₀ value of 0.82 μM, which was superior to that of osimertinib (HY-15772) (IC₅₀ = 2.94 μM), JBJ-04-125-02 (HY-135805) (IC₅₀ = 3.66 μM), and coadministration of JBJ-04-125-02 and osimertinib (IC₅₀ = 1.25 μM)^[1].

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

Chemical Information

CAS No. 3020681-05-1
Molecular Weight 624.73
Formula C₃₇H₃₆N₈O₂
SMILES

NC1=NC=CC(NC(C=C2)=CC=C2NC([C@@H](C3=CC=CC=C3)N4CC5=CC(C6=CC=C(N7CCN(CC7)C)C=C6)=CC=C5C4=O)=O)=N1
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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 (267 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]. Hu L, et al. Identification of novel aminopyrimidine derivatives for the treatment of mutant NSCLC. Eur J Med Chem. 2023 Dec 20;265:116074. [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.

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100 mg

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Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References

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EGFR-IN-97

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-97 Related Classifications

HY-157432 Related Classifications