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PF-06840003

CAT: 0013-GTR19162885-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19162885-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
A novel potent, selective, orally active, and CNS penetrant IDO-1 inhibitor with IC50 of 0.41 uM for hIDO-1; weakly inhibits hTDO-2 with IC50 of 140 uM, and shows no activity against hIDO-2 (>100 uM) ; 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) ; shown significant antitumor activity in mice and very favorable ADME profile.Brain Cancer Phase 1 Clinical (In Vitro) :PF-06840003 reverses IDO-1-induced T-cell anergy in vitro. 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.
CAS Number
198474-05-4
Product Name Alternative
PF06840003 | PF 06840003 | EOS 200271
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 28 mg/mL
Smiles
O=C (C (C1=CNC2=C1C=C (F) C=C2) C3) NC3=O
Molecular Formula
C12H9FN2O2
Molecular Weight
232.2104632
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2,5-Pyrrolidinedione, 3- (5-fluoro-1H-indol-3-yl) -

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