[CAS NO. 198474-05-4] PF-06840003
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PRODUCTS SPECIFICATIONS [198474-05-4]
Store
Catalog
SLK-S8657
Brand
Selleck
CAS
198474-05-4
DESCRIPTION [198474-05-4]
Overview
| MDL | MFCD25121820 |
|---|---|
| Molecular Weight | 232.21 |
| Molecular Formula | C12H9FN2O2 |
| SMILES | O=C(C(C1=CNC2=C1C=C(F)C=C2)C3)NC3=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3064 mL | 21.5322 mL | 43.0645 mL |
| 5 mM | 0.8613 mL | 4.3064 mL | 8.6129 mL |
| 10 mM | 0.4306 mL | 2.1532 mL | 4.3064 mL |
| 50 mM | 0.0861 mL | 0.4306 mL | 0.8613 mL |
Description
PF-06840003 (EOS200271) is a highly selective orally bioavailable inhibitor. Although it has moderate hIDO1 enzyme inhibition (IC50 0.41 μM), it is a highly efficient compound (LE 0.53, LipE 5.1), driven by its tight packing within the enzyme, as well as the high density of hydrogen bonds it forms with hIDO-1 despite its small size.
In vitro
PF-06840003 is a racemic mixture. The IC50s of PF-06840003 for hIDO-1, mouse IDO-1 and dog IDO-1 are 0.41, 1.5 and 0.59 μM, respectively. It has very weak activity against hTDO-2, with an IC50 of 140 μM. In cellular assays, 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). PF-06840003 is a very weak inhibitor of CYPs with IC50 values greater than 100 μM for most major CYP isozymes except 2C19 (IC50 value is 78 μM). Additionally, PF-06840003 does not exhibit metabolism-dependent (time-dependent and NADPH-dependent or time-dependent (NADPH-independent) inhibition of the major CYP enzymes investigated.
In vivo
PF-06840003 has a predicted half-life of 16−19 h. Oral bioavailability in the mouse and rat was 59 and 94%, respectively, and 19% in dog. PF-06840003 has shown significant antitumor activity in monotherapy in Pan02, B16−F10, CT26, MC38, 4T1, and Renca models (p < 0.05 vs vehicle-treated group) and very good synergy in combination with anti-PDL1 mAb in CT26 model (p < 0.05 vs monotherapy groups).The PK profile of the compound is excellent, with a low/moderate clearance in most preclinical species. The compound also shows good CNS penetration in rat, suggesting potential impact on brain metastases.
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