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Cat. No.: HY-190903

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YNW-1

YNW-1 is a dual-site irreversible EGFR covalent inhibitor. YNW-1 simultaneously covalently modifies the Cys775 and Cys797 residues of EGFR, thereby inhibiting multiple mutant forms of EGFR. YNW-1 inhibits p-EGFR, p-ERK, and p-AKT downstream signaling, and exhibits broad activity against Del19, T790M, C797S, exon 20 insertion, and rare EGFR mutants, with kinome selectivity. YNW-1 can be used for research related to non-small cell lung cancer.

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

CAS No.: 3097630-45-7
Formula: C₃₉H₄₅N₉O₄
Molecular Weight:703.83

Storage:

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

YNW-1 Chemical Structure

CAS No.: 3097630-45-7

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

EGFR^L858R

15.82 nM (IC₅₀)

EGFR^del19

37.69 nM (IC₅₀)

EGFR^{del19 T790M}

619.5 nM (IC₅₀)

EGFR exon 20 ASV insertion

123.2 nM (IC₅₀)

EGFR^L861Q

183.5 nM (IC₅₀)

All EGFR Isoforms :

All Akt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC50	15.82 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR L858R assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR L858R assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
BaF3	IC50	18.97 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR L858R/C775S assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR L858R/C775S assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
BaF3	IC50	62.45 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR L858R/C797S assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR L858R/C797S assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
BaF3	IC50	123.2 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR exon 20 insertion insASV assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR exon 20 insertion insASV assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
BaF3	IC50	250 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR exon 20 insertion insSVD assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR exon 20 insertion insSVD assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
BaF3	IC50	102.5 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR exon 20 insertion insFQEA assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR exon 20 insertion insFQEA assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
BaF3	IC50	68.42 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR E709K assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR E709K assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
BaF3	IC50	183.5 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR L861Q assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR L861Q assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
BaF3	IC50	65.1 nM	Antiproliferative activity against Ba/F3 cells expressing EGFR G719A/E709K assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against Ba/F3 cells expressing EGFR G719A/E709K assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as

In Vitro

YNW-1 inhibits the activity of purified EGFR L858R kinase in HTRF assays, with an apparent IC₅₀ below 10 nM; it is also selective in KINOMEscan profiling, with only 7 kinases inhibited by more than 90%^[1].
YNW-1 simultaneously forms intramolecular covalent bonds with Cys775 and Cys797 in the kinase domain of recombinant EGFR L858R^[1].
YNW‑1 exhibits proliferation-inhibitory activity against multiple EGFR-mutant Ba/F3 cells under 72 h exposure conditions, with IC₅₀ values reaching the nanomolar range for L858R-series mutations; it is effective against Del19, exon 20 insertion, and E709K, G719A/E709K and other mutations, but its activity is markedly reduced against Del19/T790M mutant cells^[1].

YNW-1 (10-1000 nM; 6 h) inhibits p-EGFR, p-ERK, and p-Akt signaling in L858R, L858R/C775S, and L858R/C797S Ba/F3 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Ba/F3 cells expressing EGFR L858R, L858R/C775S, or L858R/C797S
Concentration:

10, 50, 100, 500, 1000 nM
Incubation Time:

6 h
Result:

Suppressed p-EGFR, p-ERK, and p-Akt signaling in L858R, L858R/C775S, and L858R/C797S Ba/F3 cells.

Chemical Information

CAS No. 3097630-45-7
Molecular Weight 703.83
Formula C₃₉H₄₅N₉O₄
SMILES

O=C1N([C@@H]2CCCN(C(C=C)=O)C2)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4OC)=NC=C3C=C1N6C(C=CC=C7C)=C7N(C(C=C)=O)CC6
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

Handling Instructions (2659 KB)

References

[1]. Li Z, et al. Overcoming EGFR Resistance by Monovalent and Bident Inhibitors Targeting Cys775. ACS Central Science, 2026.

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.

Bioz

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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YNW-1

All EGFR Isoforms

All Akt Isoforms