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You are here:Home-Chemical Inhibitors & Agonists-Epigenetics-Histone Methyltransferase (HMTase)-CPI-1205
CPI-1205

Chemical Structure : CPI-1205

CAS No.: 1621862-70-1

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CPI-1205 (Lirametostat;CPI 1205;CPI1205)

Catalog No.: PC-60299Not For Human Use, Lab Use Only.

Lirametostat (CPI-1205) is a highly potent, selective EZH2 inhibitor with biochemical IC50 of 2 nM, cellular EC50 of 32 nM.

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50 mg $598 In stock
100 mg $898 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Lirametostat (CPI-1205) is a highly potent, selective EZH2 inhibitor with biochemical IC50 of 2 nM, cellular EC50 of 32 nM.
Lirametostat (CPI-1205) demonstrates modest selectivity over EZH1 (IC50=52 nM), and a clean selectivity profile against 30 other histone or DNA methyltransferases.
Lirametostat (CPI-1205) exhibits robust antitumor effects in a Karpas-422 xenograft model (at 160 mg/kg BID).

Physicochemical Properties

M.Wt 518.57
Formula C27H33F3N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide

References

1. Vaswani RG, et al. J Med Chem. 2016 Nov 10;59(21):9928-9941.

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