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CPI-169

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Catalog No.
B4678
EZH2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,280.00
现货
5mg
¥ 1,160.00
现货
10mg
¥ 1,680.00
现货
50mg
¥ 5,420.00
现货
100mg
¥ 9,450.00
现货

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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

文献引用

1. Hamid Bolouri, Mary Young, et al. "Integrative network modeling reveals mechanisms underlying T cell exhaustion." bioRxiv. 2019 March 19.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt528.66
Cas No.1450655-76-1
FormulaC27H36N4O5S
Solubility≥26.45mg/mL in DMSO
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
SDFDownload SDF
Canonical SMILESCCS(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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

各种细胞系

溶解方法

该化合物在DMSO中的溶解度>26.5mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

N/A

应用

在各种细胞系中,CPI-169抑制PRC2的催化活性,IC50值<1nM,H3507细胞水平降低,EC50值为70nM,触发细胞周期停滞和细胞凋亡。

动物实验[1]:

动物模型

EZH2突变体KARPAS-422弥漫性大B细胞淋巴瘤(DLBCL)异种移植物

剂量

200 mpk每天两次(BID); 皮下注射

应用

在EZH2突变体KARPAS-422扩散性大B细胞淋巴瘤(DLBCL)异种移植物中,CPI-169在小鼠中耐受性良好,没有观察到毒性作用或体重减轻。CPI-169治疗以剂量依赖的方式导致肿瘤生长抑制(TGI),降低药效学标记物H3K27me3的水平。最高剂量(200 mpk BID)导致完全的肿瘤消退。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

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.

质量控制

化学结构

CPI-169

相关生物数据

CPI-169