1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR VEGFR Apoptosis
  3. EGFR-IN-174

EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer.

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EGFR-IN-174

EGFR-IN-174 Chemical Structure

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Description

EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer[1].

IC50 & Target[1]

VEGFR-2

0.2007 μM (IC50)

In Vitro

EGFR-IN-174 (compound 3a) (2 days) displays strong cytotoxicity against HCT-116, HepG-2, and MCF-7 Cell Lines (IC50 = 5.58, 4.82 and 11.15 μM, respectively) coupled with minimal cytotoxicity against normal WI-38 cells (IC50 = 86.26 μM)[1].
EGFR-IN-174 (4.82-11.15 μM, 72 h) effectively induces cell cycle arrest at both the G2/M and Pre-G1 phases, and significantly triggers apoptosis in HCT-116, HepG-2, and MCF-7 Cells[1].

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

Cell Cycle Analysis[1]

Cell Line: HCT-116, HepG-2, and MCF-7 Cells
Concentration: 5.58, 4.82, and 11.15 μM for HCT-116, HepG-2, and MCF-7 Cells, respectively
Incubation Time: 72 h
Result: Induced a significant increase in the Hep-G2 cell population in the G2/M (from 12.73 % to 34.85 %) and Pre-G1 (from 1.92 % to 11.82 %) phases.
Induced a significant increase in the HCT-116 cell population in the G2/M (from 5.45 % to 29.21 %) and Pre-G1 (from 1.91 % to 11.22 %) phases.
Significantly increased the population of MCF-7 Cells in the G2/M and Pre-G1 phases from 9.55 % and 2.14 % to 35.31 % and 15.52 %, respectively.
Reduced the proportion of cells in the G0-G1 and S phases compared to the control in Hep-G2, HCT-116, and MCF-7 cell lines.

Apoptosis Analysis[1]

Cell Line: HCT-116, HepG-2, and MCF-7 Cells
Concentration: 5.58, 4.82, and 11.15 μM for HCT-116, HepG-2, and MCF-7 Cells, respectively
Incubation Time: 72 h
Result: Induced a total apoptosis rate of 11.22 % in HCT-116 cells (early: 3.62 %; late: 6.24 %).
Induced a total apoptosis rate of 11.82 % in HepG-2 cells (early: 3.59 %; late: 6.65 %).
Induced a total apoptosis rate of 15.52 % in MCF-7 cells (early: 4.49 %; late: 8.88 %).
Molecular Weight

385.57

Formula

C16H23N3O2S3

SMILES

S=C(N/N=C(C1=CC=C(S(=O)(N2CCC(C)CC2)=O)C=C1)\C)SC

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • 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.

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Product Name:
EGFR-IN-174
Cat. No.:
HY-178005
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