A potent covalent type II inhibitor against FGFR with in vitro and in vivo anti-breast cancer efficacy.
FIIN-4 is a potent, irreversible, type II inhibitor against FGFR (IC50 = 2.6, 2.6, 5.6, 9.2 nM, respectively, against FGFR1-4) whose 4-acrylamidebenzyl moiety covalently modifies FGFR P-loop cysteine in its DFG-out conformation with good target selectivity based on a 456-kinase panel (354 non-mutants kinases) kinome profiling. FIIN-4 effectively inhibits FGF2-induced Erk1/2 phosphorylation in serum-starved D2.A1 murine mammary carcinoma cells (by 100% wtih 18-hr 250 nM pretreatment) and D2.A1 growth in 3D cultures (by 54% at 100 nM) without affecting EGF-dependent Erk phosphorylation or 3D growth of NMuMG murine mammary epithelial cells. Oral administration (25 mg/kg q.o.d.) is efficacious in suppressing the growths of tumors-derived from murine mammary carcinoma 4T1 lung metastases and patient TNBC brain metastases xenografts in mice in vivo with good pharmacokinetics (Tmax = 0.5 hr, T1/2 = 2.4 hr, AUC = 935 h·ng/mL; 10 mg/kg p.o.) and without overt toxicity to the animals.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Molecular cancer therapeutics, 15(9), 2096-2106 (2016-07-03)
Therapeutic targeting of late-stage breast cancer is limited by an inadequate understanding of how tumor cell signaling evolves during metastatic progression and by the currently available small molecule inhibitors capable of targeting these processes. Herein, we demonstrate that both β3
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