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.
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- CAS 番号: 2857033-34-0
- 分子式: C19H17ClFN3O4
- 分子量:405.81
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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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.
化学情報
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CAS 番号 2857033-34-0
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分子量 405.81
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
EGFR-IN-73 関連分類
HY-151882 関連分類
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