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.
Purity & Quality Control
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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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02395601||Active not recruiting||B-Cell Lymphoma||Constellation Pharmaceuticals||March 2015||Phase 1|
|NCT03480646||Recruiting||Metastatic Castration Resistant Prostate Cancer (mCRPC)||Constellation Pharmaceuticals||November 15 2017||Phase 1|Phase 2|
|NCT03525795||Recruiting||Advanced Solid Tumors||Constellation Pharmaceuticals||December 14 2017||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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