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Pulrodemstat benzenesulfonate

Cat. No. M10727
Pulrodemstat benzenesulfonate Structure
Synonym:

CC-90011 benzenesulfonate

Size Price Availability Quantity
5mg USD 130  USD130 In stock
10mg USD 210  USD210 In stock
25mg USD 370  USD370 In stock
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Quality Control & Documentation
Biological Activity

CC-90011 benzenesulfonate is a potent, selective, reversible and orally active lysine-specific demethylase-1 (LSD1) inhibitor,IC50 0.25 nM. CC-90011 benzenesulfonate has less enzymatic inhibition of LSD2, MOA-A and MAO-B. CC-90011 benzenesulfonate induces differentiation of acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells and has potent anti-cancer activity.

Chemical Information
Molecular Weight 609.65
Formula C30H29F2N5O5S
CAS Number 2097523-60-7
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage -20°C, dry, 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] Toufike Kanouni, et al. J Med Chem. Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1)

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Keywords: Pulrodemstat benzenesulfonate, CC-90011 benzenesulfonate supplier, Histone demethylase, inhibitors, activators


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