PF-06840003
CAS No. : 198474-05-4
(Synonyms: EOS200271)
| Size | Price | Stock |
|---|---|---|
| 5mg | $60 | In-stock |
| 10mg | $110 | In-stock |
| 50mg | $160 | In-stock |
| 100mg | $250 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-101111 |
| M.Wt: | 232.21 |
| Formula: | C12H9FN2O2 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 100 mg/mL |
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[1][2]. 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)[2]. 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].
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