2311901-93-4
Chemical Structure
BAY 2476568
- CAS No.: 2311901-93-4
- Formula:C24H27FN4O4
- Molecular Weight:454.49
IUPAC Name: 3-((3-fluoro-2-methoxyphenyl)amino)-2-(3-(2-methoxy-2-methylpropoxy)pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
InChIKey: ZOEVXMKZJWZLFX-UHFFFAOYSA-N
SMILES: O=C1C2=C(NC(C3=C(OCC(C)(OC)C)C=NC=C3)=C2NC4=CC=CC(F)=C4OC)CCN1
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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BAY 2476568 | 99.88% | 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. | ||||||||||||||||||||
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- [1]. 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. [Content Brief]
- [2]. 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.
Keywords
