2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis MAPK/ERK Pathway Stem Cell/Wnt
  3. EGFR HSP PI3K Caspase Apoptosis CDK ERK Akt
  4. EGFR-IN-182

EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer.

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

EGFR-IN-182

EGFR-IN-182 Chemical Structure

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EGFR-IN-182 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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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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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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ERK ERK1 ERK2 ERK5 ERK8

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Akt Akt1 Akt2 Akt3

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Description

EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer[1].

IC50 & Target[1]

EGFR

199 nM (IC50)

HSP90

5.007 μM (IC50)

PI3K

13.596 μM (IC50)

Caspase 9

 

ERK

 

Akt

 

Molecular Weight

430.46

Formula

C25H18N8
SMILES

N1(CC2=CC=CC=C2)C3=NC(N/N=C/C4=NC(C=CC=C5)=C5N=C4)=NN=C3C6=C1C=CC=C6
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-182 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-182EGFRHSPPI3KCaspaseApoptosisCDKERKAktEpidermal growth factor receptorErbB-1HER1Heat shock proteinsPhosphoinositide 3-kinaseCyclin dependent kinaseExtracellular signal regulated kinasesPKBProtein kinase BTriazino[5,6-b]indole-hydrazonesTriazino[5,6-b]indole-fused heterocyclic hybridsEGFR enzyme inhibitionHsp90 inhibitionPI3K-AKT signalingERK/AKT signalingCaspase-9 activationIn silico docking studyCancer drug designMulti-target inhibitors in cancer therapyInhibitorinhibitorinhibit

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