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^[1].

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.

469.86

C₂₁H₁₅ClF₃NO₄S

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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• [1]. Rasha M Hassan, et al. Novel benzenesulfonamides as dual VEGFR2/FGFR1 inhibitors targeting breast cancer: Design, synthesis, anticancer activity and in silico studies. Bioorg Chem. 2024 Aug 17:152:107728.  [Content Brief]