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> EGFR mutant-IN-1

EGFR mutant-IN-1

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Cat# HY-125841

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Brand : MedChemExpress


EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).

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

EGFR mutant-IN-1 Chemical Structure

EGFR mutant-IN-1 Chemical Structure

This product is a controlled substance and not for sale in your territory.

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4
Description

EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM)[1].

IC50 & Target

IC50: 27.5 nM (EGFRL858R/T790M/C797S) and >1.0 μM (EGFRWT)[1]
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
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]

  • [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.

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EGFR mutant-IN-1 Related Classifications

  • JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  • EGFR

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR mutant-IN-1EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit