PF-06840003

SKU: orb1302966

Description

PF-06840003 (EOS200271) is a potent and selective small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with oral bioavailability. It is a research tool used in immuno-oncology to study IDO1's role in tryptophan metabolism and immune suppression in both cellular assays and in vivo models.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 198474-05-4
• MW: 232.21
• Purity: >98%
• Formula: C₁₂H₉FN₂O₂
• SMILES: Fc1ccc2[nH]cc(C3CC(=O)NC3=O)c2c1
• Target: Tryptophan
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  IDO1 (human):0.41 μM|IDO1 (mouse):1.5 μM|dIDO1:0.59 μM
• In Vivo:
  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.
• In Vitro:
  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).

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EOS200271

Compound Identifiers

PubChem CID

23063810