1. Epigenetics
  2. Epigenetic Reader Domain

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

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

CPI-169 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  

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Other Forms of CPI-169:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

CPI-169 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

IC50: 0.24 nM (EZH2 WT), 0.51 nM (EZH2 Y641N), 6.1 nM (EZH1)

In Vitro

CPI-169 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 (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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 59 mg/mL (111.60 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.
References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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CPI-169
Cat. No.:
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CPI-169

Cat. No.: HY-15956A