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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Indoleamine 2,3-Dioxygenase (IDO)-PF-06840003
PF-06840003

Chemical Structure : PF-06840003

CAS No.: 198474-05-4

PF-06840003 (PF 06840003, EOS200271)

货号: PC-42320Not For Human Use, Lab Use Only.

PF-06840003 is a novel potent, selective, orally active, and CNS penetrant IDO-1 inhibitor with IC50 of 0.41 uM for hIDO-1.

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10 mg ¥880 In stock
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50 mg ¥2280 In stock
100 mg ¥3880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-06840003 (EOS200271) is a novel potent, selective, orally active, and CNS penetrant IDO-1 inhibitor with IC50 of 0.41 uM for hIDO-1.
PF-06840003 weakly inhibits hTDO-2 with IC50 of 140 uM, and shows no activity against hIDO-2 (>100 uM).
PF-06840003 shows activity both in the HeLa assay (IC50=1.8 uM) as well as in the LPS/INFγ-stimulated THP1 cells (IC50=1.7 uM), maintains good efficiency in the whole blood assay (IC50=4.7 uM).
PF-06840003 shows significant antitumor activity in mice and very favorable ADME profile.

物理化学性质&存储条件

分子量 232.2104632
分子式 C12H9FN2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 28 mg/mL

Chemical Name/SMILES

2,5-Pyrrolidinedione, 3-(5-fluoro-1H-indol-3-yl)-

参考文献

1. Crosignani S, et al. J Med Chem. 2017 Nov 21. doi: 10.1021/acs.jmedchem.7b00974.

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