TGF-βR1/VEGFR2-IN-1
TGF-βR1/VEGFR2-IN-1 is a dual inhibitor targeting TGF-βR1/VEGFR2, with an IC50 of 232.5 nM against human TGF-βR1 and an IC50 of 371.4 nM against human VEGFR2. TGF-βR1/VEGFR2-IN-1 mediates antiproliferative effects by inhibiting the TGF-βR1 and VEGFR2 signaling pathways. TGF-βR1/VEGFR2-IN-1 can be used in research related to colorectal cancer, non-small cell lung cancer, cervical cancer, and hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Formula: C25H23F3N4O2
- Molecular Weight:468.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All VEGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
TGF-βR1 232.5 nM (IC50) |
VEGFR2 371.4 nM (IC50) |
In Vitro
TGF-βR1/VEGFR2-IN-1 (compound 3b5) (Serial dilutions; 2.5 h) inhibits recombinant TGF-βR1 kinase with an IC50 of 232.5 nM[1].
TGF-βR1/VEGFR2-IN-1 (10 μM serial dilutions; 30 min pre-incubation, 60 min reaction time) inhibits recombinant VEGFR-2 kinase with an IC50 of 371.4 nM[1].
TGF-βR1/VEGFR2-IN-1 forms stable, specific interactions with key residues in the ATP-binding clefts of both TGF-βR1 and VEGFR-2, maintaining consistent binding poses over 500 ns of MD simulation[1].
TGF-βR1/VEGFR2-IN-1 (100 μM serial dilutions; 72 h) inhibits proliferation of A549, HeLa, Bel-7402, and HT-29 human cancer cells with IC50 values of 26.4 μM, 9.9 μM, 7.8 μM, and 4.6 μM respectively, while showing minimal cytotoxicity to normal HEK-293 T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human non-small cell lung cancer A549 cells, human cervical cancer HeLa cells, human hepatocellular carcinoma Bel-7402 cells, human colorectal cancer HT-29 cells, normal human embryonic kidney HEK-293 T cells
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Concentration:Serial dilutions starting at 100 μM
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Incubation Time:72 h
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Result:Inhibited proliferation of A549 cells with an IC50 value of 26.4 μM.
Inhibited proliferation of HeLa cells with an IC50 value of 9.9 μM.
Inhibited proliferation of Bel-7402 cells with an IC50 value of 7.8 μM.
Inhibited proliferation of HT-29 cells with an IC50 value of 4.6 μM.
Showed low cytotoxicity toward normal HEK-293 T cells with an IC50 > 1000 μM.
Chemical Information
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Molecular Weight 468.47
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Formula C25H23F3N4O2
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SMILES
O=C(NC1CCCCC1)CC2=COC3=CC=C(C4=CNN=C4C5=NC(C(F)(F)F)=CC=C5)C=C23
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TGF-βR1/VEGFR2-IN-1 Related Classifications
HY-187187 Related Classifications
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