PF-06726304 acetate

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PF-06726304 acetate 

PF-06726304 acetate 是一种有效的选择性 EZH2 抑制剂。PF-06726304 acetate 抑制野生型和 Y641N 突变型 EZH2，Ki 分别为 0.7 和 3.0 nM。PF-06726304 acetate 具有强效的抗肿瘤生长活性。

PF-06726304 acetate

PF-06726304 acetate Chemical Structure

CAS No. : 2080306-28-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PF-06726304 acetate 的其他形式现货产品:

PF-06726304

生物活性

PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity[1].

IC50 & Target[1]

EZH2 WT

0.7 nM (Ki)

EZH2 Y641N

3.0 nM (Ki)

体外研究
(In Vitro)

PF-06726304 (Compound 31) inhibits H3K27me3 in Karpas-422 with an IC50 of 15 nM[1].
PF-06726304 inhibits the proliferation of Karpas-422 cells that harbor wild-type EZH2 with an IC50 of 25 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PF-06726304 (200 and 300 mg/kg; BID for 20 days) inhibits tumor growth and induces robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Scid beige mice (6-8 weeks old) with Karpas-422 xenograft model[1]
Dosage: 200 and 300 mg/kg
Administration: Given BID for 20 days
Result: Inhibited tumor growth and induced robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model.

分子量

506.38

Formula

C24H25Cl2N3O5
CAS 号

2080306-28-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Kung PP, et al. Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors. J Med Chem. 2016 Sep 22;59(18):8306-25.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务