PF-06840003|198474-05-4|(EOS200271)-陌孚医药/Medlife

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PF-06840003 (Synonyms: EOS200271)

目录号: PL01176 纯度: ≥99%

CAS No. :198474-05-4

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中文名称	PF-06840003
中文别名	3-(5-氟-吲哚-3-基)-吡咯烷-2,5-二酮;3-(5-氟-1H-吲哚-3-基)-2,5-吡咯烷二酮
英文名称	PF-06840003
英文别名	3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione;EOS200271;3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione;3-(5-Fluoro-1H-indol-3-yl)-2,5-pyrrolidinedione;2,5-Pyrrolidinedione, 3-(5-fluoro-1H-indol-3-yl)-;PF06840003;(R)-3-(5-FLUORO-1H-INDOL-3-YL)PYRROLIDINE-2,5-DIONE;(S)-3-(5-FLUORO-1H-INDOL-3-YL)PYRROLIDINE-2,5-DIONE;GTPL9565;US9603836, Compound 1a;US9603836, Compound 1;MXKLDYKORJEOPR-UHFFFAOYSA-N;BDBM309529;BCP17158;SB22834;E;PF-06840003
Cas No.	198474-05-4
分子式	C₁₂H₉FN₂O₂
分子量	232.21
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

PF-06840003 (EOS200271) 是一种有口服活性的选择性 IDO-1 抑制剂，抑制 hIDO-1， dIDO-1，和 mIDO-1 的IC₅₀ 分别为 0.41 μM， 0.59 μM，和 1.5 μM。

生物活性

PF-06840003 (EOS200271) is a highly selective orally bioavailable IDO-1 inhibitor with IC 50 s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.

性状

Solid

IC50 & Target[1][2]

IDO-1

体外研究(In Vitro)

PF-06840003 reverses IDO-1-induced T-cell anergy in vitro . PF-06840003 shows activity both in the HeLa assay (IC50=1.8 μM) as well as in the LPS/ INFγ-stimulated THP1 cells (IC50=1.7 μM). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

PF-06840003 reduces intratumoral kynurenine levels in mice by >80% and inhibits tumor growth in multiple preclinical syngeneic models in mice, in combination with immune checkpoint inhibitors. PF-0684003 has favorable predicted human pharmacokinetic properties, including a predicted t1/2 of 16-19 hours. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Tumang J, et al. PF-06840003: a highly selective IDO-1 inhibitor that shows good in vivo efficacy in combination with immune checkpoint inhibitors. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 20
[2]. Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate. J Med Chem. 2017 Dec 14;60(23):9617-9629.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (430.64 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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