FGFR1/VEGFR2-IN-2
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells.
For research use only. We do not sell to patients.
- Formula: C21H15ClF3NO4S
- Molecular Weight:469.86
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All VEGFR Isoforms
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Biological Activity
|
FGFR1 0.026 μM (IC50) |
VEGFR2 0.025 μM (IC50) |
PDGFRβ 0.077 μM (IC50) |
FGFR 0.106 μM (IC50) |
FGFR1/VEGFR2-IN-2 (10 μM) has anti-tumor proliferation activity with an average GI of 60.38%[1].
FGFR1/VEGFR2-IN-2 has good cytotoxicity against breast cancer cell lines T-47D, MCF-7 and MDA-MB-231, and has no effect on normal cells Vero[1].
FGFR1/VEGFR2-IN-2 (10, 20 μM) blocks T-47D cells in the G1 phase[1].
FGFR1/VEGFR2-IN-2 (2.12, 4.25 μM) promotes early and late apoptosis of T-47D cells and promotes cell necrosis[1].
FGFR1/VEGFR2-IN-2 (3.7-4.8 μM) promotes cell necrosis, increases the expression of BAX and Caspase-3, and decreases the expression of BCL-2[1].
FGFR1/VEGFR2-IN-2 (6 μM; 24, 48 h) has an anti-migratory effect in T-47D[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T-47D, MCF-7, MDA-MB-231, Vero
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Concentration:10 μM
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Incubation Time:
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Result:Had no cytotoxicity to Vero cells and the IC50 for T-47D was 8.51 μM, the IC50 for MCF-7 was greater than 100 μM, and the IC50 for MDA-MB-231 was 69.17 μM.
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Cell Line:NCI-60
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Concentration:10 μM
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Incubation Time:
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Result:Inhibited lung cancer (NCI-H460), colon cancer (HCC-2998), central nervous system cancer (SF-295), melanoma (UACC-62), ovarian cancer (OVCAR-5), kidney cancer (UO-31), and breast cancer (MDA-MB-231), GI were 89.11%, 81.73%, 82.33%, 97.59%, 81.63%, 87.08% and 82.85%.
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Cell Line:T-47D
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Concentration:10, 20 μM
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Incubation Time:
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Result:Increased the number of T-47D cells in the G1 phase from 60.81% to 72.62%.
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Cell Line:T-47D
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Concentration:6.0 μM
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Incubation Time:0, 24, 48 h
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Result:Increased the wound healing rate from 25.2% to 19.8% after 24 hours and from 42.2% to 31.2% after 48 hours.
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Cell Line:T-47D
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Concentration:2.12, 4.25 μM
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Incubation Time:
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Result:Increased the early apoptosis rate of T-47D cells by 25% and 20% at 2.12 and 4.25 μM, and the late apoptosis rate by 10% and 16%. At 2.12 μM, the apoptosis rate increased by 8%, and at 4.25 μM, the apoptosis rate increased by 16%. At 2.12 and 4.25 μM, the necrotic cells increased from 5% to 12%.
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Cell Line:T-47D
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Concentration:1/2 × IC50 (T-47D), IC50=8.5 μM
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Incubation Time:
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Result:Increased the expression level of BAX by 5.82 times, decreased the expression level of BCL-2 by 0.243 times, and increased the expression level of Caspase-3 by 8.2 times.
Chemical Information
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Molecular Weight 469.86
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Formula C21H15ClF3NO4S
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SMILES
ClC1=CC=C(C(COC2=CC=C(NS(C3=CC=C(C(F)(F)F)C=C3)(=O)=O)C=C2)=O)C=C1
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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)