FIIN-4

FIIN-4

Biochem/physiol Actions

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.

No detailed specifications are available for this product.

There are no downloads for this product.

Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575615 FIIN-4 white to beige 100 SIGMA-ALDRICH 2-8°C DMSO: 10 mg/mL, clear powder ≥98% (HPLC)
£391.39 (exc VAT) per 25MG
-
+
3575616 FIIN-4 white to beige 100 SIGMA-ALDRICH 2-8°C DMSO: 10 mg/mL, clear powder ≥98% (HPLC)
£119.37 (exc VAT) per 5MG
-
+