CPI-1205( CPI 1205 | CPI1205 )

Catalog No. M12387 CAS No. 1621862-70-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

CPI-1205
Note

Research use only, not for human use.
Brief Description

A highly potent, selective EZH2 inhibitor with biochemical IC50 of 2 nM, cellular EC50 of 32 nM.
Description

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

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In Vivo

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Synonyms

CPI 1205 | CPI1205
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

Cancer
Indication

Prostate Cancer

CAS Number

1621862-70-1
Formula Weight

518.57
Molecular Formula

C27H33F3N4O3
Purity

>98% (HPLC)
Solubility

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SMILES

C[C@@H](N1C2=C(C(C(NCC3=C(C=C(NC3=O)C)OC)=O)=C1C)C=CC=C2)C4CCN(CC(F)(F)F)CC4
Chemical Name

(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

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

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