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CPI-360 

Cat. No.: HY-15955 Purity: 99.14%
Handling Instructions

CPI-360 is a potent, selectiveEZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively.

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

CPI-360 Chemical Structure

CPI-360 Chemical Structure

CAS No. : 1802175-06-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 238 In-stock
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2040 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Validation

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

CPI-360 is a potent, selective EZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively. IC50 value: 0.5 nM, 2.5 nM Target: EZH2 in vitro: CPI-360 functions on the basis of S-adenosyl-Lmethionine (SAM)-competition, inhibits EZH1 about 100-fold less and shows exquisite selectivity across a large panel of histone lysine and arginine, and DNA methyltransferases. CPI-360 potently reduced global H3K27me3 and H3K27me2 levels in a dosedependent manner. CPI-360 effectively suppressed heavy H3K27me3 incorporation in KARPAS-422 cells without affecting total histone turnover. CPI-360 treatment causes time-dependent transcriptional changes in germinal center B cell-like diffuse large B cell lymphoma. in vivo: Twice daily, subcutaneous administration of 200 mg/kg of CPI-360 reduced tumor growth (TGI 44%) of KARPAS-422 xenografts in mice without affecting body weight or causing any overt adverse effects. CPI-360 completely inhibits EZH2 catalytic activity, since we entirely suppress H3K27me3 turnover over time.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 48.9 mg/mL (111.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2856 mL 11.4278 mL 22.8556 mL
5 mM 0.4571 mL 2.2856 mL 4.5711 mL
10 mM 0.2286 mL 1.1428 mL 2.2856 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

437.53

Formula

C₂₅H₃₁N₃O₄

CAS No.

1802175-06-9

SMILES

CC(N1)=CC(OC)=C(CNC(C2=C(C)N([[email protected]](C)C3CCOCC3)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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Product Name:
CPI-360
Cat. No.:
HY-15955
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CPI-360

Cat. No.: HY-15955