CAS 1802175-06-9|CPI-360

Introduction：Basic information about CAS 1802175-06-9|CPI-360, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. CPI-360 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	CPI-360
CAS Number	1802175-06-9	Molecular Weight	437.531
Density	1.3±0.1 g/cm3	Boiling Point	712.2±60.0 °C at 760 mmHg
Molecular Formula	C₂₅H₃₁N₃O₄	Melting Point	/
MSDS	/	Flash Point	384.5±32.9 °C

Names

Name	N-[(4-Methoxy-6-methyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-1H-indole-3-carboxamide
Synonym	More Synonyms

CPI-360 BiologicalActivity

Description	CPI-360 is a potent, selective EZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively.IC50 value: 0.5 nM, 2.5 nMTarget: EZH2in vitro: CPI-360 functions on the basis of S-adenosyl-Lmethionine(SAM)-competition, inhibits EZH1 about 100-fold less and shows exquisite selectivity across a large panel of histone lysine and arginine, and DNA methyltransferases. CPI-360 potently reduced global H3K27me3 and H3K27me2 levels in a dosedependent manner. CPI-360 effectively suppressed heavy H3K27me3 incorporation in KARPAS-422 cells without affecting total histone turnover. CPI-360 treatment causes time-dependent transcriptional changes in germinal center B cell-like diffuse large B cell lymphoma.in vivo: Twice daily, subcutaneous administration of 200 mg/kg ofCPI-360 reduced tumor growth (TGI 44%) of KARPAS-422 xenografts in mice without affecting body weight or causing any overt adverse effects. CPI-360 completely inhibits EZH2 catalytic activity, since we entirely suppress H3K27me3 turnover over time.
Related Catalog	Signaling Pathways >>Epigenetics >>Epigenetic Reader DomainResearch Areas >>Cancer
References	[1]. Bradley WD, et al. EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation. Chem Biol. 2014 Nov 20;21(11):1463-1475. [2]. Bruno NC, et al. Design and Preparation of New Palladium Precatalysts for C-C and C-N Cross-Coupling Reactions. Chem Sci. 2013;4:916-920.

Description

CPI-360 is a potent, selective EZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively.IC50 value: 0.5 nM, 2.5 nMTarget: EZH2in vitro: CPI-360 functions on the basis of S-adenosyl-Lmethionine(SAM)-competition, inhibits EZH1 about 100-fold less and shows exquisite selectivity across a large panel of histone lysine and arginine, and DNA methyltransferases. CPI-360 potently reduced global H3K27me3 and H3K27me2 levels in a dosedependent manner. CPI-360 effectively suppressed heavy H3K27me3 incorporation in KARPAS-422 cells without affecting total histone turnover. CPI-360 treatment causes time-dependent transcriptional changes in germinal center B cell-like diffuse large B cell lymphoma.in vivo: Twice daily, subcutaneous administration of 200 mg/kg ofCPI-360 reduced tumor growth (TGI 44%) of KARPAS-422 xenografts in mice without affecting body weight or causing any overt adverse effects. CPI-360 completely inhibits EZH2 catalytic activity, since we entirely suppress H3K27me3 turnover over time.

Related Catalog

Signaling Pathways >>Epigenetics >>Epigenetic Reader DomainResearch Areas >>Cancer

References

[1]. Bradley WD, et al. EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation. Chem Biol. 2014 Nov 20;21(11):1463-1475.

[2]. Bruno NC, et al. Design and Preparation of New Palladium Precatalysts for C-C and C-N Cross-Coupling Reactions. Chem Sci. 2013;4:916-920.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	712.2±60.0 °C at 760 mmHg
Molecular Formula	C₂₅H₃₁N₃O₄
Molecular Weight	437.531
Flash Point	384.5±32.9 °C
Exact Mass	437.231445
LogP	2.20
Vapour Pressure	0.0±2.3 mmHg at 25°C
Index of Refraction	1.621
InChIKey	PFPSFENQCNMITC-MRXNPFEDSA-N
SMILES	COc1cc(C)[nH]c(=O)c1CNC(=O)c1c(C)n(C(C)C2CCOCC2)c2ccccc12
Storage condition	-20℃

Synonyms

N-[(4-Methoxy-6-methyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-1H-indole-3-carboxamide

1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-

CPI-360

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