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Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
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 | FGFR:0.106 μM, FGFR1:0.026 μM, PDGFRβ:0.077 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. |
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