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Bomedemstat

Cat. No. M29081
Bomedemstat Structure
Synonym:

IMG-7289

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Biological Activity

Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.

Chemical Information
Molecular Weight 519.61
Formula C28H34FN7O2
CAS Number 1990504-34-1
Form Oil
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
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] Ivan Krecak, et al. Curr Hematol Malig Rep. Advances in Risk Stratification and Treatment of Polycythemia Vera and Essential Thrombocythemia

[2] Joseph B Hiatt, et al. Clin Cancer Res. Inhibition of LSD1 with Bomedemstat Sensitizes Small Cell Lung Cancer to Immune Checkpoint Blockade and T-Cell Killing

[3] Douglas Tremblay, et al. Int J Hematol. Novel treatments for myelofibrosis: beyond JAK inhibitors

[4] Samantha Hodges, et al. Cancer Rep (Hoboken). Novel lysine-specific histone demethylase 1 inhibitor in acute myeloid leukaemia transformed from essential thrombocythaemia

[5] Douglas Tremblay, et al. Cells. Next Generation Therapeutics for the Treatment of Myelofibrosis

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  Catalog
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Keywords: Bomedemstat, IMG-7289 supplier, Histone demethylase, inhibitors, activators


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