2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. 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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EGFR-IN-73 Chemical Structure

EGFR-IN-73 Chemical Structure

CAS No. : 2857033-34-0

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EGFR-IN-73 Related Antibodies

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Description

EGFR-IN-73 (Compound 3f) is a potent inhibitor for the most common EGFR mutation EGFR Del19 with an IC50 of 119 nM[1].

IC50 & Target[1]

EGFRdel19

119 nM (IC50)

EGFRL858R

820 nM (IC50)

EGFRWT

>10 μM (IC50)

EGFRL858R/T790M

>10 μM (IC50)

In Vitro

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.

EGFR-IN-73 Related Antibodies

Cell Proliferation Assay[1]

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
Concentration: 0.01 nM-10 μM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells expressing various EGFR mutants
Concentration: 10, 100 and 1000 nM
Incubation Time: 8 h
Result: Showed significant activity at L858R and excellent activity at the Del19 and Del19/C797S mutant EGFR. Did not affect T790M and WT EGFR.
Molecular Weight

405.81

Formula

C19H17ClFN3O4
CAS No.
SMILES

COC1=C2C=C(C(NC3=CC(Cl)=C(F)C=C3OCCOCCO2)=NC=N4)C4=C1
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
References
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EGFR-IN-73 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR-IN-732857033-34-0EGFREpidermal growth factor receptorErbB-1HER1Del19L858RBa/F3Inhibitorinhibitorinhibit

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HY-151882
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