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Romidepsin (FK228)

Cat. No. M2007
Romidepsin (FK228) Structure
Synonym:

FK228; ISTODAX; Depsipeptide; FR 901228; NSC 630176

Size Price Availability Quantity
1mg USD 110  USD110 In stock
5mg USD 300  USD300 In stock
10mg USD 535  USD535 In stock
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Quality Control & Documentation
Biological Activity

Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a structurally unique, potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM, respectively. Romidepsin inhibits the growth of U-937, K562, and CCRF-CEM cells with IC50 of 5.92 nM, 8.36 nM, and 6.95 nM, respectively. Romidepsin exhibits concentration-dependent cytotoxicity against a panel of mantle cell lymphoma (MCL) cell lines. FK228 (Romidepsin) treatment potently inhibits the neovascularization of chick embryo and that of adult mice in the Matrigel plug assay. FK228(Romidepsin) is currently in a Phase I study in treating patients with lymphoma, chronic lymphocytic leukemia, or solid tumors with liver dysfunction.<span style='color:#ff0000;'><strong>*The compound is unstable in solutions, freshly prepared is recommended</strong></span>


Product Citations
Chemical Information
Molecular Weight 540.7
Formula C24H36N4O6S2
CAS Number 128517-07-7
Solubility (25°C) DMSO 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Coiffier B, et al. J Clin Oncol. Results from a pivotal, open-label, phase II study of romidepsin in relapsed or refractory peripheral T-cell lymphoma after prior systemic therapy.

[2] Piekarz RL, et al. Blood. Phase 2 trial of romidepsin in patients with peripheral T-cell lymphoma.

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Keywords: Romidepsin (FK228), FK228; ISTODAX; Depsipeptide; FR 901228; NSC 630176 supplier, HDAC, inhibitors, activators

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