Cell lines

Human NB cell ( SMS-KCNR, SK-N-BE2, SH-SY5Y, SK-N-AS, L A1-15N, SH-SHEP and IMR32 lines)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Reaction Conditions

72h; IC50 ranged from 1–6.5 ng/ml

Applications

Romidepsin (0.5–30 ng/mL) resulted in a dose-dependent decrease in cell viability of all NB cell lines as measured by the MTT or MTS assay. The romidepsin IC50 ranged from 1–6.5 ng/ml in different NB cell lines. Morphological examination by light microscopy revealed that all of the NB cell lines treated with romidepsin had a dose-dependent decrease in cell number and extensive change in morphology to rounded, denser and non-adherent cells.

Animal models

Normal and nude mice

Dosage form

1.0-10kg/mL; i.v.; the tail injection

Applications

Clolon 38 and Colon 26 were implanted sc and M5076 and Meth A were implanted id in mice on Day 0. When the drug were given beginning on Day 1. romidepsin markedly inhibited the growth of Colon 38 and M5076, but not Colon26 or Meth A. In addition, when the drug were given beginning on Day 4, or on 7 or 8, romidepsin potently inhibited the growth of Colon 38, M5076 and Meth A, and its activities against M5076 and Meth A were potent than when it was given beginning on Day 1.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Romidepsin, also known as FK228 or depsipeptide, is potent and selective inhibitor of histone deacetylases (HDACs) which are associated with the regulation of re-expression of silenced tumor suppressor genes. It was the first HDAC inhibitor to manifest anti-tumor activity and originally isolated from a rod-shaped Gram-negative bacterium, Chromobacterium violaceum, found in a Japanese soil sample. Romidepsin exhibits a stronger inhibition towards HDAC1 and HDAC2 enzymes (class I), removing acetyl groups from the lysine residues of N-terminal histone tails and maintaining a more open and transcriptionally active chromatin state, than HDAC4 and HDAC6 enzymes (class II). Besides HDAC inhibition, romidepsin is also able to induce cell cycle arrest, cellular differentiation, apoptosis and alteration of gene expression in adult malignancies.

Reference

[1].Karen M VanderMolen, William McCulloch, Cedric J Pearce and Nicholas H Oberlies. Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma. The Journal of Antibiotics 2011: 64, 525-531
[2].Jyoti Panicker, Zhijie Li, Christine McMahon, Caroline Sizer, Kenneth Steadman, Richard Piekarz, Susan E. Bates and Carol J. Thiele. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells. Cell Cycle 2010 9:9, 1830-1838