1. Epigenetics
  2. Histone Methyltransferase
  3. CPI-169

CPI-169 (Synonyms: CPI 169 R-enantiomer)

Cat. No.: HY-15956A Purity: 96.99%
Handling Instructions

CPI-169 (CPI 169 R-enantiomer) is a novel and potent EZH2 inhibitor, with IC50s of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

For research use only. We do not sell to patients.

CPI-169 Chemical Structure

CPI-169 Chemical Structure

CAS No. : 1802175-07-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 488 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of CPI-169:

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Description

CPI-169 (CPI 169 R-enantiomer) is a novel and potent EZH2 inhibitor, with IC50s of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

IC50 & Target[2]

EZH2 WT

0.24 nM (IC50)

EZH2 Y641N

0.51 nM (IC50)

EZH1

6.1 nM (IC50)

In Vitro

CPI-169 (CPI 169 R-enantiomer) inhibits the catalytic activity of PRC2 with an IC50 of < 1nM, decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines[1]. 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[2].

In Vivo

CPI-169 (CPI 169 R-enantiomer) (200 mpk, s.c. BID) is well tolerated in mice with no observed toxic effect or body weight loss. CPI-169 treatment leads to tumor growth inhibition (TGI) of an EZH2 mutant KARPAS-422 DLBCL xenograft. CPI-169 (100 mpk, BID) with a single dose of CHOP leads tumors to rapidly regress and become unpalpable[1]. 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[2].

Molecular Weight

528.66

Formula

C₂₇H₃₆N₄O₅S

CAS No.

1802175-07-0

SMILES

CC(N1)=CC(OC)=C(CNC(C2=C(C)N([[email protected]](C)C3CCN(S(=O)(CC)=O)CC3)C4=CC=CC=C24)=O)C1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (189.16 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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 3.7832 mL
10 mM 0.1892 mL 0.9458 mL 1.8916 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

CPI-169CPI 169 R-enantiomerCPI169CPI 169Histone MethyltransferaseInhibitorinhibitorinhibit

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CPI-169
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HY-15956A
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