Decitabine is a potent DNA methyltransferase inhibitor with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively. Decitabine is a hypomethylating agent. It hypomethylates DNA by inhibiting DNA methyltransferase. The DNA methyltransferase inhibitor Decitabine is able to reactivate genes silenced by DNA methylation and has been shown to be a very potent epigenetic compound in several hematological malignancies. Decitabine exhibits high antineoplastic activity against anaplastic large cell lymphoma (ALCL), a rare CD30 positive non-Hodgkin lymphoma of T-cell origin. The combination of Decitabine with TSA or depsi produced a greater inhibition of growth and DNA synthesis and a greater loss of clonogenicity than either agent alone. Decitabine is highly efficient against ALCL and warrants further clinical evaluation for future therapeutic use. In clinical trials, Decitabine was demonstrated to be an active antileukemic agent.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 40 mg/mL|
Antineoplastic activity of the DNA methyltransferase inhibitor 5-aza-2'-deoxycytidine in anaplastic large cell lymphoma.
Hassler MR, et al. Biochimie. 2012 Nov;94(11):2297-307. PMID: 22687603.
Decitabine improves patient outcomes in myelodysplastic syndromes: results of a phase III randomized study.
Kantarjian H, et al. Cancer. 2006 Apr 15;106(8):1794-803. PMID: 16532500.
Pharmacology of 5-Aza-2'-deoxycytidine (decitabine).
Momparler RL. Semin Hematol. 2005 Jul;42(3 Suppl 2):S9-16. PMID: 16015507.
Results of decitabine (5-aza-2'deoxycytidine) therapy in 130 patients with chronic myelogenous leukemia.
Kantarjian HM, et al. Cancer. 2003 Aug 1;98(3):522-8. PMID: 12879469.
|Related DNA Methyltransferase Products|
Vitamin D2 is a selective inhibitor of mammalian DNA polymerase A (pol A) with IC50 of 123 mM.
SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B
RG108 is a novel small-molecule inhibitors of DNA methyltransferases with IC50 of 115 nM.
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