Revision 1

#48132Store at -20C

5 mg

Cell Signaling Technology

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For Research Use Only. Not for Use in Diagnostic Procedures.

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).

  1. Krämer, A. et al. (2013) Nat Chem Biol 9, 731-8.
  2. Gan, R.H. et al. (2019) Onco Targets Ther 12, 7663-7674.
  3. Zhang, M. et al. (2020) Cell Death Dis 11, 981.
  4. Lu, Z. et al. (2018) Biomed Pharmacother 107, 1370-1376.

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

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 week to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Directions for Use

FLI-06 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 1.14 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

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

    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
    All other trademarks are the property of their respective owners. Visit cellsignal.com/trademarks for more information.

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    Revision 1
    #48132

    FLI-06

    FLI-06: Image 1 Expand Image
    FLI-06 的化学结构。