|(S)-4-(1-(3-(二氟甲基)-1-甲基-5-(3-(三氟甲基)苯氧基)-1H-吡唑-4-甲酰胺基)乙基)苯甲酸|CsnPharm

CAS No.: 1369489-71-3

Palupiprant Catalog No. CSN21111

Synonyms: E7046

E7046 is a specific antagonist of the type 4 prostaglandin E2 (PGE2) receptor EP4. It possesses significant antitumor growth activity in multiple preclinical tumor models through modulating myeloid cells, including tumor-associated macrophages and myeloid-derived suppressor cells.

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400-920-2911

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tech@csnpharm.cn

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生物活性

实验方案

技术信息

生物活性

描述The EP4 prostanoid receptor is one of four receptor subtypes for prostaglandin E2, which belongs to the family of G protein-coupled receptors. EP4 signaling plays a variety of roles through cAMP effectors, i.e., protein kinase A and exchange protein activated by cAMP^[1]. E7046 is a newly developed and highly specific EP4 antagonist with IC₅₀ of 13.5 nM and with a >1500 fold selectivity for EP4 relative to the PGE₂ receptor EP2. E7046 reversed the immunosuppressive effects of PGE₂ on activation and differentiation of human myeloid cells through selective EP4 antagonism. In murine BM-derived haematopoietic cells induced to differentiate into CD11c-expressing DCs, E7046 antagonism of PGE₂ effects on BM cell differentiation rescued T cell proliferation in response to TCR activation in a dose-dependent manner. Daily oral administration of 150 mg/kg E7046 was found to inhibit the growth of multiple syngeneic tumor models: fibrosarcoma SaI/N, pancreatic PAN02, colon CT26, and breast EMT6 and 4T1^[2].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03152370	Neoadjuvant Therapy in Rectal ... more >>Cancer Collapse <<	Phase 1	Recruiting	January 2019	United States, Massachusetts ... more >> Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 United States, New York Weill Cornell Recruiting New York, New York, United States, 10065 Poland Marie-Skodowska Curie Cancer Centre Recruiting Warsaw, Poland United Kingdom The Christie Recruiting Manchester, United Kingdom Mount Vernon Hospital Recruiting Northwood, United Kingdom Collapse <<
NCT02540291	Tumors	Phase 1	Terminated(Terminated due to, ... more >>licensing agreement granting exclusive rights of research, development, manufacture and marketing of Eisai's E7046 to Adlai Nortye Biopharma.) Collapse <<	-	United States, Massachusetts ... more >> Boston, Massachusetts, United States United States, Texas Houston, Texas, United States France Villejuif, Cedex, France Collapse <<

参考文献

[1] Yokoyama U, Iwatsubo K, Umemura M, Fujita T, Ishikawa Y. The prostanoid EP4 receptor and its signaling pathway. Pharmacol Rev. 2013;65(3):1010-1052. Published 2013 Jun 17.
[2] Albu DI, Wang Z, Huang KC, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. Oncoimmunology. 2017;6(8):e1338239. Published 2017 Jun 28.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0687 mL
- 10.3437 mL
- 20.6873 mL
- 5 mM
- 0.4137 mL
- 2.0687 mL
- 4.1375 mL
- 10 mM
- 0.2069 mL
- 1.0344 mL
- 2.0687 mL

技术信息

CAS号

1369489-71-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H18F5N3O4

运输

蓝冰

分子量

483.39

别名

E7046

溶解度

DMSO	170.0 mg/mL (351.7 mM)
Water	insoluble

动物实验配方

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