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.
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- CAS No.: 3097630-45-7
- Formule: C39H45N9O4
- Masse moléculaire:703.83
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
EGFRL858R 15.82 nM (IC50) |
EGFRdel19 37.69 nM (IC50) |
EGFRdel19 T790M 619.5 nM (IC50) |
EGFR exon 20 ASV insertion 123.2 nM (IC50) |
EGFRL861Q 183.5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
15.82 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| BaF3 | IC50 |
18.97 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| BaF3 | IC50 |
62.45 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| BaF3 | IC50 |
123.2 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| BaF3 | IC50 |
250 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| BaF3 | IC50 |
102.5 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| BaF3 | IC50 |
68.42 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| BaF3 | IC50 |
183.5 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| BaF3 | IC50 |
65.1 nM
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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.
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acscentsci.6c01219?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
In Vitro
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.
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Cell Line:Ba/F3 cells expressing EGFR L858R, L858R/C775S, or L858R/C797S
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Concentration:10, 50, 100, 500, 1000 nM
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Incubation Time:6 h
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Result:Suppressed p-EGFR, p-ERK, and p-Akt signaling in L858R, L858R/C775S, and L858R/C797S Ba/F3 cells.
Chemical Information
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CAS No. 3097630-45-7
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Masse moléculaire 703.83
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Formule C39H45N9O4
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YNW-1 Related Classifications
HY-190903 Related Classifications
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Keywords
- YNW-1
- 3097630-45-7
- YNW1
- YNW 1
- EGFR
- PERK
- Akt
- Epidermal growth factor receptor
- ErbB-1
- HER1
- Protein kinase R-like endoplasmic reticulum kinase
- PKR-like endoplasmic reticulum kinase
- PKB
- Protein kinase B
- ATP-binding pocket
- Cys775
- Cys797
- acquired EGFR resistance mutations
- mutant EGFR
- non-small cell lung cancer
- p-AKT
- p-EGFR
- p-ERK
- Inhibitor
- inhibitor
- inhibit