PF-06726304 acetate

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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

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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.

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