GlpBio

CPI-169

目录号: GC16599纯度: >98.00%
A selective EZH2 inhibitor
CPI-169
Cas No.: 1450655-76-1
规格价格库存数量操作
5mg¥945.00现货
1
10mg¥1,418.00现货
1
50mg¥5,376.00现货
1
100mg¥9,051.00现货
1
10mM (in 1mL DMSO)¥2,877.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

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

实验参考方法 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
1450655-76-1
化学名
(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
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
分子式
C27H36N4O5S
分子量
528.66 g/mol
溶解性
≥ 26.45mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol