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PF-06840003

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

IDO1|IDO|Indoleamine 2,3-Dioxygenase (IDO)|Indoleamine 2,3-Dioxygenase|Indoleamine 2,3Dioxygenase (IDO)|Indoleamine2,3Dioxygenase|Indoleamine2,3Dioxygenase(IDO)|inhibit|EOS200271|EOS-200271|EOS 200271|Inhibitor|PF06840003|PF-06840003|PF 06840003

验证数据展示

  • CAS No.: 198474-05-4

    PF-06840003
    CAS#: 198474-05-4

产品信息

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|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 | Shipping with blue ice.
别名 IDO1|IDO|Indoleamine 2,3-Dioxygenase (IDO)|Indoleamine 2,3-Dioxygenase|Indoleamine 2,3Dioxygenase (IDO)|Indoleamine2,3Dioxygenase|Indoleamine2,3Dioxygenase(IDO)|inhibit|EOS200271|EOS-200271|EOS 200271|Inhibitor|PF06840003|PF-06840003|PF 06840003

靶点活性

IDO1 (human):0.41 μM|IDO1 (mouse):1.5 μM|dIDO1:0.59 μM

体内活性

在小鼠中，PF-06840003能显著降低肿瘤内kynurenine水平（>80%）。在多项小鼠同源移植模型的前临床研究中，PF-06840003联合免疫检查点抑制剂可有效抑制肿瘤生长。此外，PF-06840003还展现出了良好的人类药代动力学预测属性，包括预测的半衰期为16-19小时。

体外活性

PF-06840003对hIDO-1（IC50：0.41 μM）、mouse IDO-1（IC50：1.5 μM）及dog IDO-1（IC50：0.59 μM）均显示出抑制活性，但对hTDO-2的抑制作用非常弱（IC50：140 μM）。在细胞测试中，PF-06840003在LPS/INFγ刺激的THP1细胞（IC50：1.7 μM）和HeLa测试中（IC50：1.8 μM）均展现出活性。除了对2C19（IC50：78 μM）有一定的抑制效果外，PF-06840003对CYPs的抑制作用非常弱（IC50>100 μM）。

溶解度

DMSO:60 mg/mL (258.39 mM)

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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