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BAY 2476568

BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD) . BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations[1][2].

Product Specifications

CAS Number

2311901-93-4

UNSPSC

12352005

Target

Akt; EGFR; ERK

Type

Reference compound

Related Pathways

JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bay-2476568.html

Purity

99.88

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1C2=C(NC(C3=C(OCC(C)(OC)C)C=NC=C3)=C2NC4=CC=CC(F)=C4OC)CCN1

Molecular Formula

C24H27FN4O4

Molecular Weight

454.49

References & Citations

[1]Siegel F, Siegel S, Graham K, et al. Abstract 1470: preclinical activity of the first reversible, potent and selective inhibitor of EGFR exon 20 insertions. Cancer Res 2021; 81: 1470.|[2]Zhao H, et al. Biochemical analysis of EGFR exon20 insertion variants insASV and insSVD and their inhibitor sensitivity. Proc Natl Acad Sci U S A. 2024 Nov 5;121 (45) :e2417144121.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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