PF-06840003 free base · Synonyms: EOS200271

PF-06840003 is a highly selective, orally active and brain-penetrant IDO-1 inhibitor.

For research use only. Not for human or veterinary use.

Target Indoleamine 2,3-Dioxygenase (IDO)

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

PF-06840003 structure

CAS No.: 198474-05-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 450.00	BP-02488-250mg	In stock	Get quote
500 mg	USD 720.00	BP-02488-500mg	In stock	Get quote
1 g	USD 1,150.00	BP-02488-1g	In stock	Get quote
2 g	USD 1,840.00	BP-02488-2g	In stock	Get quote
3 g	USD 2,210.00	BP-02488-3g	In stock	Get quote
5 g	USD 2,950.00	BP-02488-5g	In stock	Get quote
10 g	USD 4,720.00	BP-02488-10g	In stock	Get quote

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Description

PF-06840003 (EOS200271) is a highly selective, orally active and brain-penetrant IDO-1 inhibitor with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively .

Biological activity

In Vitro PF-06840003 reverses IDO-1-induced T-cell anergy in vitro[1]. 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). 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.

Identifiers

SMILES: FC1=CC2=C(NC=C2C2CC(=O)NC2=O)C=C1
InChIKey: MXKLDYKORJEOPR-UHFFFAOYSA-N

Specifications

MW (average): 232.2105
Formula: C₁₂H₉FN₂O₂
CAS No.: 198474-05-4
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[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].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.

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