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CPI-169

(CAS No:1450655-76-1)
CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
CAS No:1450655-76-1
Molecular Weight(MW):528.66
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1450655-76-1
Molecular formula(MF) C27H36N4O5S
Molecular Weight(MW): 528.66
Alias
Solubility
In vitro DMSO 100 mg/mL (189.15 mM)
Ethanol 100 mg/mL (189.15 mM)
Water <1 mg/mL
In vivo 10% DMSO+60% PEG 400+30% ddH2O 30mg/mL
Biological Activity
Description CPI-169 is a potent, and selective EZH2 inhibitor with IC50 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. [1]

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. [1]