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Cat. No.: HY-125841

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EGFR mutant-IN-1

EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFR^{L858R/T790M/C797S} mutant inhibitor with an IC₅₀ of 27.5 nM, while being a significantly less potent for EGFR^WT (IC₅₀ >1.0 μM).

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

Formula: C₃₄H₃₉ClFN₇O₂
Molecular Weight:632.17

Storage:

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

Data Sheet (268 KB)

EGFR mutant-IN-1 Chemical Structure

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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
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 27.5 nM (EGFR^{L858R/T790M/C797S}) and >1.0 μM (EGFR^WT)^[1]

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.662 μM Compound: 8r-B	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 31298540]

Chemical Information

Molecular Weight 632.17
Formula C₃₄H₃₉ClFN₇O₂
SMILES

O=C1C(C2=CC=CC(F)=C2Cl)=C(C)C3=CN=C(NC4=CC=C(N5CCN(C)CC5)C(C)=C4)N=C3N1[C@H]6CN(C(CC)=O)CCC6
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 (268 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]. Shen J, et al. Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type SparingInhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFRL858R/T790M/C797S). J Med Chem. 2019 Aug 8;62(15):7302-7308. [Content Brief]

Calculators

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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
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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EGFR mutant-IN-1

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR mutant-IN-1 Related Classifications

HY-125841 Related Classifications