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PF-06840003

Names

[ CAS No. ]:
198474-05-4

[ Name ]:
PF-06840003

[Synonym ]:
PF-06840003
PF06840003

Biological Activity

[Description]:

PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Indoleamine 2,3-Dioxygenase (IDO)
Research Areas >> Cancer

[Target]

IDO-1


[In Vitro]

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

[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[1].

[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.


[Related Small Molecules]

Epacadostat(INCB024360) | Indoximod | Linrodostat (BMS-986205) | NLG919 | Coptisine chloride | Navoximod | INCB024360 analogue | GNF-PF-3777 | IDO-IN-4 | IDO-IN-1 | IDO-IN-12 | IDO-IN-2 | IDO-IN-3 | IDO-IN-11

Chemical & Physical Properties

[ Molecular Formula ]:
C12H9FN2O2

[ Molecular Weight ]:
232.21000

[ Exact Mass ]:
232.06500

[ PSA ]:
65.45000

[ LogP ]:
1.71300

[ Storage condition ]:
-20℃

Synthetic Route

Precursor & DownStream

Precursor

DownStream


Related Compounds

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