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CPI-169

CPI-169

Catalog No.

B4678

EZH2 inhibitor

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Grouped product items
Size	Price	Stock
10mM (in 1mL DMSO)	$128.00	In stock
5mg	$116.00	In stock
10mg	$168.00	In stock
50mg	$542.00	In stock
100mg	$945.00	In stock

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Email: [email protected]

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Background
Product Citation
Chemical Properties
Protocol
Quality Control

Background

CPI-169 is a novel, small molecule and potent inhibitor of enhancer of zeste homolog 2 (EZH2) with an IC50 value of <1nM for polycomb repressive complex 2 (PRC2) [1].

CPI-169 has been found to be a potent EZH2 inhibitor with an IC50 value of <1nM for polycomb repressive complex 2 (PRC2). In addition, CPI-169 has been reported to reduce cellular levels of histone H3 on lysine 27(H3K27) with an EC50 value of 70nM. Moreover, CPI-169 has been exhibited to trigger cell cycle arrest and apoptosis in cells. Apart from these, treatment the inhibitor at 200mpk twice daily, CPI-169 has been noted to have a well tolerated in mice with no observed toxic effect or body weight loss [1].

References:
[1] Vidya Balasubramanian, Priya Iyer, Shilpi Arora, Patrick Troyer, Emmanuel Normant. Constellation Pharmaceuticals, Cambridge, MA. CPI-169, a novel and potent EZH2 inhibitor, synergizes with CHOP in vivo and achieves complete regression in lymphoma xenograft models

Product Citation

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	528.66
Cas No.	1450655-76-1
Formula	C₂₇H₃₆N₄O₅S
Solubility	≥26.45 mg/mL in DMSO; insoluble in H2O; ≥2.18 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name	(R,Z)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((2-hydroxy-4-methoxy-6-methylpyridin-3-yl)methyl)-2-methyl-1H-indole-3-carbimidic acid
SDF	Download SDF
Canonical SMILES	CCS(N1CCC([C@@](N2C(C)=C(/C(O)=N/CC(C(O)=N3)=C(OC)C=C3C)C4=CC=CC=C42)([H])C)CC1)(=O)=O
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:
Cell lines	a variety of cell lines
Preparation method	The solubility of this compound in DMSO is >26.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	N/A
Applications	In a variety of cell lines, CPI-169 inhibited the catalytic activity of PRC2 with IC50 value of < 1nM, decreased cellular levels of H3K27me3 with EC50 value of 70 nM, and triggered cell cycle arrest and apoptosis.
Animal experiment [1]:
Animal models	EZH2 mutant KARPAS-422 diffuse large B-cell lymphoma (DLBCL) xenograft
Dosage form	200 mpk twice daily (BID); administered subcutaneously
Application	In EZH2 mutant KARPAS-422 diffuse large B-cell lymphoma (DLBCL) xenograft, CPI-169 is well tolerated in mice with no observed toxic effect or body weight loss. CPI-169 treatment led to tumor growth inhibition (TGI) in a dose-dependent way and reduced the pharmacodynamic marker H3K27me3. The highest dose (200 mpk BID) led to complete tumor regression.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1] Vidya Balasubramanian, Priya Iyer, Shilpi Arora, Patrick Troyer, Emmanuel Normant. Constellation Pharmaceuticals, Cambridge, MA. CPI-169, a novel and potent EZH2 inhibitor, synergizes with CHOP in vivo and achieves complete regression in lymphoma xenograft models.