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Givinostat hydrochloride

Cat. No. M29087
Givinostat hydrochloride Structure
Synonym:

ITF-2357 hydrochloride

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Quality Control & Documentation
Biological Activity

Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.

Chemical Information
Molecular Weight 457.95
Formula C24H28ClN3O4
CAS Number 199657-29-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Paulina Pawelec, et al. Int J Mol Sci. Analysis of Givinostat/ITF2357 Treatment in a Rat Model of Neonatal Hypoxic-Ischemic Brain Damage

[2] Michael J Topper, et al. Cell. Epigenetic Therapy Ties MYC Depletion to Reversing Immune Evasion and Treating Lung Cancer

[3] Antonio Furlan, et al. Mol Med. Pharmacokinetics, safety and inducible cytokine responses during a phase 1 trial of the oral histone deacetylase inhibitor ITF2357 (givinostat)

[4] Rainer Glauben, et al. Mol Med. Inhibition of histone deacetylases in inflammatory bowel diseases

[5] Alessandro Rambaldi, et al. Br J Haematol. A pilot study of the Histone-Deacetylase inhibitor Givinostat in patients with JAK2V617F positive chronic myeloproliferative neoplasms

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  Catalog
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Keywords: Givinostat hydrochloride, ITF-2357 hydrochloride supplier, HDAC, inhibitors, activators


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