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CPI-360

Catalog No. T6810 CAS 1802175-06-9

Synonyms: CPI360, CPI 360

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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CPI-360, CAS 1802175-06-9

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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&IC50	EZH1:102.3 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]
In vivo	In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1]

Synonyms	CPI360, CPI 360
Molecular Weight	437.54
Formula	C25H31N3O4
CAS No.	1802175-06-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 16 mg/mL (36.6 mM)

H2O: <1 mg/mL

Ethanol: 15 mg/mL (34.3 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Bradley WD, et al. Chem Biol. 2014, 21(11), 1463-1475.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CPI-360 1802175-06-9 表观遗传凋亡 Apoptosis Histone Methyltransferase CPI360 CPI 360 Inhibitor inhibitor inhibit

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