Background
The dihydropyridine FLI-06 is a Notch pathway inhibitor with an EC50 of 2.5 mM. Signaling through Notch transmembrane receptor proteins plays an important role in cell-fate decisions; aberrant Notch activity can result in cancer and other developmental disorders. FLI-06 acts at an early stage in the secretory pathway, disrupting the Golgi and inhibiting general secretion before exit from the endoplasmic reticulum (1). Studies show that FLI-06 suppresses both the mRNA and protein expression of Notch receptor and Notch targeted genes. FLI-06 treatment of tongue cancer cells inhibits Notch signaling activation, decreasing cell proliferation, blocking cell cycle arrest, and inducing apoptosis. FLI-06 inhibited tumor growth and increased cell apoptosis in a xenograft mouse model, suggesting that FLI-06 is a potential chemotherapeutic agent for the clinical treatment of tongue tumors (2). Additional studies showed that FLI-06 inactivated Notch signaling and suppressed malignant functions in lung adenocarcinoma and esophageal squamous cell carcinoma (3,4).
Molecular Formula
C25H30N2O5
Molecular Weight
438.5 g/mol
Purity
>98%
CAS
313967-18-9
Solubility
Soluble in DMSO at 50 mg/mL or ethanol at 10 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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