CPI-360

Catalog No.S7656

CPI-360 Chemical Structure

Molecular Weight(MW): 437.53

CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.

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Biological Activity

Description CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
Targets
EZH1 [1]
102.3 nM
In vitro

In KARPAS-422 cells, CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells M2i1WGZ2dmO2aX;uJIF{e2G7 Mke0O|IhcA>? NV3pZlNPUW6qaXLpeIlwdiCxZjDFXmgzKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEh|S{K3cYU{KGyndnXsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDFUGlUSSCvZYToc4QtKEmFNUC9NE4xPzVizszN MlHRNlYyQDlyN{i=

... Click to View More Cell Line Experimental Data

In vivo In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Mice bearing KARPAS-422 tumors
  • Formulation: 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2O
  • Dosages: 200 mg/kg, twice daily
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL warmed (45.71 mM)
Ethanol 18 mg/mL warmed (41.14 mM)
Water Insoluble
In vivo Add solvents individually and in order:
10% DMSO+60% PEG 400+ddH2O
20mg/mL

* 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.

Chemical Information

Molecular Weight 437.53
Formula

C25H31N3O4

CAS No. 1802175-06-9
Storage powder
Synonyms N/A

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Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID