| Description | Selective tryptophan 2, 3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). Exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. Reduces growth of TDO-expressing P815 mastocytoma tumors in mice. Orally bioavailable. |
| Target activity | TDO (mouse):2 μM, TDO (human):0.62 μM |
| molecular weight | 229.21 |
| Molecular formula | C11H8FN5 |
| CAS | 1316695-35-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | Ethanol: 4.58 mg/mL (20 mM) DMSO: 70 mg/mL (305.4 mM) |
| References | 1. Pilotte L,etal.Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase.Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502. 2. Huang W,etal.Crystal structure of Drosophila melanogaster tryptophan 2,3-dioxygenase reveals insights into substrate recognition and catalytic mechanism.J Struct Biol. 2013 Mar;181(3):291-9. |