>>Signaling Pathways>> Chromatin/Epigenetics>> Histone Methyltransferase>>CPI-169

CPI-169

Catalog No.GC16599

EZH2 inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

CPI-169 Chemical Structure

Cas No.: 1450655-76-1

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$282.00
재고 있음
5mg
US$93.00
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10mg
US$139.00
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50mg
US$527.00
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100mg
US$888.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

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.

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

Chemical Properties

Cas No. 1450655-76-1 SDF
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
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
Formula C27H36N4O5S M.Wt 528.66
Solubility ≥ 26.45mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.8916 mL 9.4579 mL 18.9157 mL
5 mM 0.3783 mL 1.8916 mL 3.7831 mL
10 mM 0.1892 mL 0.9458 mL 1.8916 mL
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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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