EGFR-IN-73
EGFR-IN-73 (Compound 3f) is a potent inhibitor for the most common EGFR mutation EGFR Del19 with an IC50 of 119 nM.
For research use only. We do not sell to patients.
- CAS No.: 2857033-34-0
- Formula: C19H17ClFN3O4
- Molecular Weight:405.81
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All EGFR Isoforms
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Biological Activity
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EGFRdel19 119 nM (IC50) |
EGFRL858R 820 nM (IC50) |
EGFRWT >10 μM (IC50) |
EGFRL858R/T790M >10 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
147.9 nM
Compound: 3f
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Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
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[PMID: 36384036] |
| BaF3 | IC50 |
197.5 nM
Compound: 3f
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Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
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[PMID: 36384036] |
| BaF3 | IC50 |
385.6 nM
Compound: 3f
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Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
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[PMID: 36384036] |
| BaF3 | IC50 |
749.6 nM
Compound: 3f
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Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
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[PMID: 36384036] |
EGFR-IN-73 (Compound 3f) (0.01 nM-10 μM; 72 h) is weakly active on the EGFR WT and a potent binder of the EGFR mutants EGFR d746-750 (Del19), EGFR d747-752/P753S, EGFR L858R, or EGFR d752-759 in addition to weaker interaction detected for other oncogenic mutants (FLT3 D835Y and FLT3 ITD D835V)[1].
EGFR-IN-73 shows excellent chemical stability under acid conditions with more than 95% after 3 h and also good stability at pH 7.4 above 80%[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 cell, EGFR WT, L858R, L858R/C797S, L858R/T790M, L858R/T790M/C797S, Del19, Del19/C797S, Del19/T790M, Del19/T790M/C797S, and Ex20 insertion mutants
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Concentration:0.01 nM-10 μM
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Incubation Time:72 h
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Result:Did not inhibit EGFR WT growth, whereas inhibited both L858R and L858R/C979S mutants in the sub-micromolar range, with IC50 values of 385.6 and 749.6 nM, respectively. Was even more potent in cells transduced with the Del19 and Del19/C797S mutations than on the other mutants in this series, with IC50 values of 197.5 and 147.9 nM, respectively.
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Cell Line:Ba/F3 cells expressing various EGFR mutants
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Concentration:10, 100 and 1000 nM
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Incubation Time:8 h
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Result:Showed significant activity at L858R and excellent activity at the Del19 and Del19/C797S mutant EGFR. Did not affect T790M and WT EGFR.
Chemical Information
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CAS No. 2857033-34-0
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Molecular Weight 405.81
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Formula C19H17ClFN3O4
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SMILES
COC1=C2C=C(C(NC3=CC(Cl)=C(F)C=C3OCCOCCO2)=NC=N4)C4=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR-IN-73 Related Classifications
HY-151882 Related Classifications
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