Cat. No.: HY-134877

BAY 2476568

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Based on 1 Customer Validation

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.

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

Purity: 99.88%
CAS No.: 2311901-93-4
Formula: C₂₄H₂₇FN₄O₄
Molecular Weight:454.49

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BAY 2476568 Chemical Structure

CAS No.: 2311901-93-4

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(In Japan)

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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
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All EGFR Isoforms :

All ERK Isoforms :

All Akt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	12.8 nM Compound: BAY 2476568	Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 48 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 48 hrs by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	IC₅₀	397 nM Compound: BAY 2476568	Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 48 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 48 hrs by Cell Titer-Glo assay	[PMID: 37669428]

In Vitro

BAY 2476568 exhibits potent inhibitory activity against EGFR exon20 insertion mutants L858R, insASV, insSVD, and insNPG, with IC₅₀ values of 28.3 nM, 0.09 nM, 0.21 nM, and 0.11 nM, respectively and shows no significant inhibitory activity against wild-type (WT) EGFR kinase, with an IC₅₀ value >1000 nM^[1].
BAY 2476568 (72 h) exerts potent antiproliferative activity against Ba/F3 cells expressing EGFR insASV and insSVD mutants, with IC₅₀ values of 24 nM and 20 nM, respectively and shows weak antiproliferative activity against Ba/F3 cells expressing WT EGFR, with an IC₅₀ value of 128 nM^[1].
BAY 2476568 (100 nM, 6 h) significantly inhibits phosphorylation of EGFR (Y1068), ERK1/2, and Akt (S473) in Ba/F3 cells expressing EGFR insASV and insSVD mutants^[1].
BAY 2476568 (100 nM, 6 h) only incompletely inhibits EGFR (Y1068) phosphorylation and weakly reduces ERK1/2 and Akt (S473) phosphorylation in Ba/F3 cells expressing WT EGFR^[1].

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

Cell Viability Assay^[1]

Cell Line:

Ba/F3 cells expressing EGFR insASV and insSVD mutants
Concentration:

100 nM
Incubation Time:

6 h
Result:

Inhibited phosphorylation of EGFR (Y1068), ERK1/2, and Akt (S473) in Ba/F3 cells expressing EGFR insASV and insSVD mutants.

Chemical Information

CAS No. 2311901-93-4
Appearance Solid
Molecular Weight 454.49
Formula C₂₄H₂₇FN₄O₄
Color Off-white to light yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (220.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2003 mL

11.0013 mL

22.0027 mL

5 mM

0.4401 mL

2.2003 mL

4.4005 mL

10 mM

0.2200 mL

1.1001 mL

2.2003 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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]. 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.

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2003 mL	11.0013 mL	22.0027 mL	55.0067 mL
	5 mM	0.4401 mL	2.2003 mL	4.4005 mL	11.0013 mL
	10 mM	0.2200 mL	1.1001 mL	2.2003 mL	5.5007 mL
	15 mM	0.1467 mL	0.7334 mL	1.4668 mL	3.6671 mL
	20 mM	0.1100 mL	0.5501 mL	1.1001 mL	2.7503 mL
	25 mM	0.0880 mL	0.4401 mL	0.8801 mL	2.2003 mL
	30 mM	0.0733 mL	0.3667 mL	0.7334 mL	1.8336 mL
	40 mM	0.0550 mL	0.2750 mL	0.5501 mL	1.3752 mL
	50 mM	0.0440 mL	0.2200 mL	0.4401 mL	1.1001 mL
	60 mM	0.0367 mL	0.1834 mL	0.3667 mL	0.9168 mL
	80 mM	0.0275 mL	0.1375 mL	0.2750 mL	0.6876 mL
	100 mM	0.0220 mL	0.1100 mL	0.2200 mL	0.5501 mL

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BAY 2476568

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

MAPK Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

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Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

All EGFR Isoforms

All ERK Isoforms

All Akt Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BAY 2476568 Related Classifications

Cat. No.: HY-134877