[CAS NO. 1450655-76-1] CPI-169

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PRODUCTS SPECIFICATIONS [1450655-76-1]

Catalog

SLK-S7616

Brand

Selleck

CAS

1450655-76-1

DESCRIPTION [1450655-76-1]

Overview

MDL	-
Molecular Weight	528.66
Molecular Formula	C27H36N4O5S
SMILES	C(C)(N1C=2C(C(C(NCC3=C(OC)C=C(C)NC3=O)=O)=C1C)=CC=CC2)C4CCN(S(CC)(=O)=O)CC4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8916 mL	9.4579 mL	18.9157 mL
5 mM	0.3783 mL	1.8916 mL	3.7831 mL
10 mM	0.1892 mL	0.9458 mL	1.8916 mL
50 mM	0.0378 mL	0.1892 mL	0.3783 mL

Description

CPI-169 is a potent, and selective inhibitor with of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

Targets

EZH2 WT ^[1]	EZH2 Y641N ^[1]	EZH1 ^[1]
0.24 nM	0.51 nM	6.1 nM

In vitro

In KARPAS-422 cells, CPI-169 shows a dose-dependent inhibitory effect on cell viability, and produces synergy anti-proliferative activity when used in combination with ABT-199. In 16 out of 25 NHL cell lines, CPI-169 also suppresses cell growth with GI50 of <5 μM.

In vivo

In mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects.

References

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

Synonyms

1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-1-[1-[1-(ethylsulfonyl)-4-piperidinyl]ethyl]-2-methyl-

N-[(1,2-Dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-1-[1-[1-(ethylsulfonyl)-4-piperidinyl]ethyl]-2-methyl-1H-indole-3-carboxamide

1-(1-(1-(Ethylsulfonyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide

CPI 169

1-[1-(1-Ethylsulfonylpiperidin-4-yl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methylindole-3-carboxamide