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INCB059872

Cat. No. M45256
INCB059872 Structure
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Biological Activity

INCB059872 is a potent, orally active, selective and irreversible inhibitor of lysine-specific demethylase 1 (LSD1) in myeloid leukemia.

Chemical Information
Molecular Weight 386.53
Formula C23H34N2O3
CAS Number 1802909-49-4
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] Stephin Baby, et al. ACS Chem Biol. Lysine-Specific Demethylase 1 (LSD1) Inhibitors: Peptides as an Emerging Class of Therapeutics

[2] Chaofeng Zhang, et al. Bioorg Chem. Recent advances of LSD1/KDM1A inhibitors for disease therapy

[3] Beatrice Noce, et al. Front Pharmacol. LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

[4] Yuan Fang, et al. J Hematol Oncol. LSD1/KDM1A inhibitors in clinical trials: advances and prospects

[5] Xiaoli Fu, et al. Future Med Chem. Advances toward LSD1 inhibitors for cancer therapy

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Keywords: INCB059872 supplier, Histone demethylase, inhibitors, activators


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