Catalog No.S8353 Synonyms: CPI 1205, CPI1205
Molecular Weight(MW): 518.57
CPI-1205 is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.
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Choose Selective Histone Methyltransferase Inhibitors
|Description||CPI-1205 is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.|
Treatment with EZH2 inhibitor CPI-1205 cause apoptosis in multiple myeloma and plasmacytoma cell models.
|In vivo||CPI-1205 shows excellent oral bioavailability. It was well-tolerated for repeat dosing as demonstrated by the absence of significant body weight loss. CPI-1205 shows relatively high clearance in both rats and dogs (3.19 L/h/kg and 1.41 L/h/kg, respectively) but demonstrates good oral bioavailability in both species(44.6% F in rats and 46.2% F in dogs). CPI-1205 was well-tolerated in the 28-day GLP toxicology studies, and any findings were reversible over the recovery period.|
|In vitro||DMSO||100 mg/mL (192.83 mM)|
|Ethanol||100 mg/mL (192.83 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||CPI 1205, CPI1205|
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