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FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.
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| Description | FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells. |
| Targets&IC50 | FGFR1:0.026 μM, PDGFRβ:0.077 μM, FGFR:0.106 μM, VEGFR2:0.025 μM |
| In vitro | FGFR1/VEGFR2-IN-2 exhibits anti-tumor proliferative activity with an average GI of 60.38% at a concentration of (10 μM). This compound demonstrates significant cytotoxicity in breast cancer cell lines T-47D, MCF-7, and MDA-MB-231 but does not affect the normal Vero cells. At concentrations of (10, 20 μM), FGFR1/VEGFR2-IN-2 induces cell cycle arrest in the G1 phase in T-47D cells. Additionally, at (2.12, 4.25 μM), it promotes early and late apoptosis in T-47D cells, as well as necrosis. Furthermore, at (3.7-4.8 μM), it augments necrosis while increasing the expression of BAX and Caspase-3, and reducing BCL-2 expression. Importantly, at (6 μM; 24, 48 h), it possesses anti-migratory effects in T-47D cells. |
| Molecular Weight | 469.86 |
| Formula | C21H15ClF3NO4S |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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