CAS NO: | 1369489-71-3 |
生物活性 | Palupiprant (E7046) is an orally bioavailable and specificEP4antagonist, withIC50of 13.5 nM andKiof 23.14 nM. Palupiprant exhibits anti-tumor activities[1][2]. | ||||||||||||||||
IC50& Target[2] |
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体外研究 (In Vitro) | Palupiprant (E7046) reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells through selective EP4 antagonism[2]. | ||||||||||||||||
体内研究 (In Vivo) | In the CT-26 tumor model, the Palupiprant/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of Palupiprant and RT also produces significant better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors[1]. Palupiprant (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. Blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. Palupiprant treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells. Furthermore, co-administration of Palupiprant and E7777, an IL-2-diphtheria toxin fusion protein that preferentially kills Tregs, synergistically disrupts the myeloid and Treg immunosuppressive networks, resulting in effective and durable anti-tumor immune responses in mouse tumor models[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 483.39 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H18F5N3O4 | ||||||||||||||||
CAS 号 | 1369489-71-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(206.87 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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