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Decitabine

Cat. No. M2052
Decitabine Structure
Synonym:

5-Aza-2'-deoxycytidine; NSC 127716; 5-AZA-CdR

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 36  USD36 In stock
10mg USD 52  USD52 In stock
25mg USD 90  USD90 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Chemical Information
Molecular Weight 228.21
Formula C8H12N4O4
CAS Number 2353-33-5
Solubility (25°C) DMSO 30 mg/mL
Water ≥10 mg/mL
Storage -20°C, protect from light, sealed
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] Hassler MR, et al. Biochimie. Antineoplastic activity of the DNA methyltransferase inhibitor 5-aza-2'-deoxycytidine in anaplastic large cell lymphoma.

[2] Kantarjian H, et al. Cancer. Decitabine improves patient outcomes in myelodysplastic syndromes: results of a phase III randomized study.

[3] Momparler RL. Semin Hematol. Pharmacology of 5-Aza-2'-deoxycytidine (decitabine).

[4] Kantarjian HM, et al. Cancer. Results of decitabine (5-aza-2'deoxycytidine) therapy in 130 patients with chronic myelogenous leukemia.

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Keywords: Decitabine, 5-Aza-2'-deoxycytidine; NSC 127716; 5-AZA-CdR supplier, DNA Methyltransferase, inhibitors, activators


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