1. Protein Tyrosine Kinase/RTK Apoptosis JAK/STAT Signaling PI3K/Akt/mTOR
  2. VEGFR Apoptosis EGFR mTOR
  3. 4-TCPA

4-TCPA is a potent VEGFR2 inhibitor. 4-TCPA induces apoptosis and cell cycle arrest, likely through inhibition of VEGFR2 and EGFR signaling with additional effects on the mTOk pathway. 4-TCPA can inhibit the vitality and proliferation of various cancer cell lines. 4-TCPA can be used for the study of cancers such as lung cancer, breast cancer and leukemia.

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

4-TCPA Chemical Structure

4-TCPA Chemical Structure

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Description

4-TCPA is a potent VEGFR2 inhibitor. 4-TCPA induces apoptosis and cell cycle arrest, likely through inhibition of VEGFR2 and EGFR signaling with additional effects on the mTOk pathway. 4-TCPA can inhibit the vitality and proliferation of various cancer cell lines. 4-TCPA can be used for the study of cancers such as lung cancer, breast cancer and leukemia[1].

IC50 & Target[1]

VEGFR2

 

mTOR

 

In Vitro

4-TCPA (0-200 μM, 72 h) 4-TCPA exhibits inhibitory activity with IC50s of 35.70 μM for A549, 19.50 μM for MCF7, 5.95 μM for K562 and 135.2 μM for HFF2 cells[1].
4-TCPA (5.95-35.70 μM, 72 h) activates the mitochondrial pathway with varying sensitivity, causing apoptotic cell death in K562, MCF7 and A549 cell lines[1].

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

Cell Proliferation Assay[1]

Cell Line: K562, MCF7, A549 and HFF2 cells
Concentration: 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200 μM
Incubation Time: 72 h
Result: Demonstrated a dose- and time-dependent decrease in the viability and proliferation of cell lines.
Exhibited nearly twofold more activity in producing cytotoxic effects on the cancer cell line.
Was somewhat hazardous to the regular HFF2 cell line.

Apoptosis Analysis[1]

Cell Line: K562, MCF7, A549 cells
Concentration: 5.95, 19.50, 35.70 μM
Incubation Time: 72 h
Result: The early and late apoptosis in all cell lines increased significantly with time.
More than 40% of the treated cells underwent apoptosis.
Increased the activity of caspase 3/7 in a time-dependent manner.

RT-PCR[1]

Cell Line: K562, MCF7, A549 and HFF2 cells
Concentration: 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200 μM
Incubation Time: 72 h
Result: Decreased the levels of EGFR, VEGFR2 and mTOR in A549.
Decreased the levels of EGFR, VEGFR2, mTOR, MAPK-1 and PIK3CA in MCF7.
Decreased the levels of EGFR, VEGFR2, mTOR, MAPK-1 and Akt in K562.
Molecular Weight

541.99

Formula

C25H28ClN7O5

SMILES

O=C(NC1=CC=C(Cl)C=C1)CN2N=NC(CNC3=C4C=C(OCCOC)C(OCCOC)=CC4=NC=N3)=C2

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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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.

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Product Name:
4-TCPA
Cat. No.:
HY-175220
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