2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis Bcl-2 Family Caspase
  4. EGFR-IN-186

EGFR-IN-186 is a potent inhibitor of EGFR with an IC50 of 0.065 µM. EGFR-IN-186 also exhibits inhibitory activity against EGFRL858R (IC50 = 0.528 µM) and EGFRT790M (IC50 = 0.465 µM). EGFR-IN-186 induces apoptosis by increasing Bax and caspase-3 levels and down-regulating Bcl-2 expression level. EGFR-IN-186 can be used for the research of non-small cell lung cancer (NSCLC).

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

EGFR-IN-186

EGFR-IN-186 Chemical Structure

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EGFR-IN-186 Related Antibodies

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

EGFR-IN-186 is a potent inhibitor of EGFR with an IC50 of 0.065 µM. EGFR-IN-186 also exhibits inhibitory activity against EGFRL858R (IC50 = 0.528 µM) and EGFRT790M (IC50 = 0.465 µM). EGFR-IN-186 induces apoptosis by increasing Bax and caspase-3 levels and down-regulating Bcl-2 expression level. EGFR-IN-186 can be used for the research of non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

EGFR

0.065 μM (IC50)

EGFRL858R

0.528 μM (IC50)

EGFRT790M

0.465 μM (IC50)

In Vitro

EGFR-IN-186 (compound 6) (48 h) exhibits potent cytotoxicity against A549, NCI-H460, and HOP-62 cancer cell lines (IC50 = 4.55, 26.09, and 10.72 μM, respectively), while showing significantly lower toxicity toward the normal human lung fibroblast cell line WI-38 (IC50 = 44.64 μM)[1].
EGFR-IN-186 (48 h) exhibits enhancement in its cytotoxicity against A-549 cells (IC50 = 2.38 μM after radiation), indicating that it shows a good radiosensitizing ability[1].
EGFR-IN-186 (4.55 μM; 48 h) induces apoptosis through increasing Bax and caspase-3 levels and down-regulating Bcl-2 expression level in A549 cells[1].

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

EGFR-IN-186 Related Antibodies

Apoptosis Analysis[1]

Cell Line: A-549
Concentration: 4.55 μM
Incubation Time: 48 h
Result: Caused a remarkable increase in early apoptosis from 0.79% (control) to 18.51%.
Showed an increase in the late cellular apoptosis from 0.18% (control) to 6.57%.
Induced early apoptosis in A-549 cells 1.65 folds better than Erlotinib (HY-50896).

ELISA Assay[1]

Cell Line: A-549
Concentration: 4.55 μM
Incubation Time: 48 h
Result: Increased the level of pro-apoptotic protein Bax expression compared to control.
Down-regulated the level of the expression of anti-apoptotic protein Bcl-2 compared to control.
Increased the Bax/BCl-2 ratio.
Led to activation of caspase-3 and increased its expression level when compared to untreated control cells.
Molecular Weight

472.52

Formula

C24H20N6O3S
SMILES

O=C(NC=N1)C2=C1N(C=C2C3=CC=CC=C3)C4=CC=C(S(=O)(NC5=NC(C)=CC(C)=N5)=O)C=C4
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-186 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-186EGFRApoptosisBcl-2 FamilyCaspaseEpidermal growth factor receptorErbB-1HER1Lung cancerMolecular dockingInhibitorinhibitorinhibit

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