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CPI-169 racemate

🥰Excellent
Catalog No. T6809Cas No. 1450655-76-1
Alias CPI-169, CPI169, CPI 169

CPI-169 racemate (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.

CPI-169 racemate

CPI-169 racemate

🥰Excellent
Purity: 99.14%
Catalog No. T6809Alias CPI-169, CPI169, CPI 169Cas No. 1450655-76-1
CPI-169 racemate (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.
Pack SizePriceAvailabilityQuantity
1 mg$51In Stock
2 mg$72In Stock
5 mg$127In Stock
10 mg$180In Stock
25 mg$396In Stock
50 mg$589In Stock
100 mg$839In Stock
1 mL x 10 mM (in DMSO)$148In Stock
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Purity:99.14%
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Product Introduction

Bioactivity
Description
CPI-169 racemate (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&IC50
EZH2 (Y641N):0.51 nM, EZH2 (WT):0.24 nM, EZH1:6.1 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]
Kinase Assay
Biochemical Assays: Compound potency is also assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, PRC2 containing either EZH1 (160 pM), wt EZH2 (40 pM), or Y641N mutant EZH2 (80 pM, both EZH2 prepared in-house) is pre-incubated with 3H-SAM (0.9 μM), 2 μM H3K27me3 activating peptide (H2N-RKQLATKAAR(Kme3)SAPATGGVKKP-amide) and compounds (as 10 point duplicate dose response titrations) for 120 min in a buffer consisting of 50 mM Tris (pH 8.5), 1 mM DTT, 0.07 mM Brij-35, 0.1% BSA, and 0.8% DMSO in a total volume of 12.5 μl in a black 384 well plate. Reaction is initiated with biotinylated H3 substrate peptides (H3K27me1 for wt EZH2, H3K27me2 for Y641N mutant EZH2; H2N-RKQLATKAAR(Kmen)SAPATGGVKKP-NTPEGBiot) as a 2 μM stock in 12.5 μL and allowed to react at room temperature for 5 h. Quenching is accomplished by addition of 20 μl of STOP solution (50 mM Tris (pH 8.5), 200 mM EDTA, 2 mM SAH). 35 μL of the quenched solution is transferred to Streptavidin Flashplates, incubated overnight, washed, and read in a TopCount Reader. For titrations all compound dilutions are in DMSO, final DMSO concentrations are 0.8% (v/v), and turnover is kept to less than < 5%. IC50s are calculated using non-linear least square four parameter fits (GraphPad 6.0).
Cell Research
Relative cell numbers are assessed by Cell Titer-Glo (CTG) luminescent cell viability assay using an Envision instrument. GraphPad Prism 6.0 is used for curve fitting, IC50/GI50 and Hill coefficient (H) calculations. The GI90 is calculated using the formula: EC90 = (90 /100-90)1/H * EC50.(Only for Reference)
Animal Research
Animal Models: Mice bearing KARPAS-422 subcutaneous xenograftsFormulation: 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2ODosages: 200 mg/kg, BIDAdministration: s.c.
AliasCPI-169, CPI169, CPI 169
Chemical Properties
Molecular Weight528.66
FormulaC27H36N4O5S
Cas No.1450655-76-1
SmilesCCS(=O)(=O)N1CCC(CC1)C(C)n1c(C)c(C(=O)NCc2c(OC)cc(C)[nH]c2=O)c2ccccc12
Relative Density.1.31 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 93 mg/mL (175.9 mM)
DMSO: 93 mg/mL (175.9 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.8916 mL9.4579 mL18.9157 mL94.5787 mL
5 mM0.3783 mL1.8916 mL3.7831 mL18.9157 mL
10 mM0.1892 mL0.9458 mL1.8916 mL9.4579 mL
20 mM0.0946 mL0.4729 mL0.9458 mL4.7289 mL
50 mM0.0378 mL0.1892 mL0.3783 mL1.8916 mL
100 mM0.0189 mL0.0946 mL0.1892 mL0.9458 mL

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