VEGFR-2/AKT-IN-2
VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells.
For research use only. We do not sell to patients.
- Formula: C25H16FN5S
- Molecular Weight:437.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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VEGFR2 0.061 μM (IC50) |
Bcl-2 |
Caspase 3 |
VEGFR-2/AKT-IN-2 has similar VEGFR2 (on the HepG-2 cell) inhibitory activity with an IC50 value of 0.061 μM compared to Sorafenib (HY-10201) [1].
VEGFR-2/AKT-IN-2 (0.39-100 μM, 48 h) inhibits the growth of HepG-2 and HuH-7 cell lines with IC50 of 0.75 and 3.43 μM, respectively, whereas the IC50 for THLE-2 is 25.53 μM[1].
VEGFR-2/AKT-IN-2 (0.75 μM) reduces both total VEGFR2 and p-VEGFR2 in treated HepG-2 cells by 38.32 % and 77.64 %, respectively[1].
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) reduces total and phosphorylated AKT in HepG-2 cells, respectively[1].
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) promotes apoptosis with increasing the percentage of early and late apoptotic cells (from 0.39% to 26.28% and from 0.21% to 18.87%, respectively), up-regulating BAX and caspase-3, and down-regulating Bcl-2[1].
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) prevents the progression of HepG-2 cell cycle during S phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG-2, HuH-7, THLE-2
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Concentration:100 μM, 25 μM, 6.25 μM, 1.56 μM, and 0.39 μM.
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Incubation Time:48 h
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Result:Inhibited the growth of HepG-2 and HuH-7 cell lines with IC50 of 0.75 μM and 3.43 μM, respectively.
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Cell Line:HepG-2
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Concentration:0.75 μM
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Incubation Time:48 h
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Result:The cell cycle progression was arrested during the S phase in 48.02% of HepG-2 cells compared to untreated HepG-2 cells (29.66%).
Significantly decreased the proportion of cells in the G2/M phase (58.71%) and increased the proportion of cells in the S phase after 24 h.
Chemical Information
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Molecular Weight 437.49
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Formula C25H16FN5S
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SMILES
CC1=CC=C(C=C1)C2=CSC(N/N=C3C4=NC5=CC=C(C=C5N=C4C6=C/3C=CC=C6)F)=N2
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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)
VEGFR-2/AKT-IN-2 Related Classifications
HY-169431 Related Classifications
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