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PF-06840003

PF-06840003 (EOS200271) 是口服具有活力的、选择性的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。

CAS号

198474-05-4

分子式

C12H9FN2O2

主要靶点

IDO|Indoleamine 2,3-Dioxygenase (IDO)

仅限科研使用

Cat No : CM04704

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Synonyms

EOS200271|PF 06840003

验证数据展示

  • CAS No.: 198474-05-4

    PF-06840003
    CAS#: 198474-05-4

产品信息

PF-06840003 (EOS200271) is a specific and oral active IDO-1 inhibitor.

CAS号 198474-05-4
分子式 C12H9FN2O2
主要靶点 IDO|Indoleamine 2,3-Dioxygenase (IDO)
主要通路 代谢
分子量 232.21
纯度 99.89%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 EOS200271|PF 06840003

靶点活性

hIDO-1:0.41 μM|mIDO-1:1.5 μM|dIDO-1:0.59 μM

体内活性

In mice, PF-06840003 reduces intratumoral kynurenine levels (>80%). In multiple preClinicalal syngeneic models in mice, It inhibits tumor growth by combinated with immune checkpoint inhibitors. PF-0684003 has favorable predicted human pharmacokinetic properties, including a predicted t1/2 of 16-19 hours.

体外活性

The s of PF-06840003 has inhibitory for hIDO-1 (IC50: 0.41 μM), mouse IDO-1 (IC50: 1.5 μM) and dog IDO-1 (IC50: 0.59 μM), respectively. It has very weak inhibitory against hTDO-2 (IC50: 140 μM). In cellular assays, PF-06840003 shows activity both in the LPS/INFγ-stimulated THP1 cells (IC50: 1.7 μM) and in the HeLa assay (IC50: 1.8 μM). PF-06840003 is a very weak inhibitory against CYPs (IC50>100 μM) except 2C19 (IC50: 78 μM).

溶解度

DMSO:28 mg/mL

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; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr4863.
2.Nguyen D J M, Theodoropoulos G, Li Y Y, et al. Targeting the kynurenine pathway for the treatment of cisplatin resistant lung cancer[J]. Molecular Cancer Research. 2019: molcanres. 0239.2019.
3.Nguyen D J M, Theodoropoulos G, Li Y Y, et al. Targeting the kynurenine pathway for the treatment of cisplatin-resistant lung cancer[J]. Molecular Cancer Research. 2020, 18(1): 105-117.

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