Biological Activity
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.
Technical Data
M. Wt | 229.21 |
Formula | C11H8FN5 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1316695-35-8 |
PubChem ID | 91885138 |
InChI Key | FSGAFWYMLAWNJM-UHFFFAOYSA-N |
Smiles | FC1=CC=C2C(NC=C2/C=C/C3=NN=NN3)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 22.92 | 100 | |
ethanol | 4.58 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 229.21. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 4.36 mL | 21.81 mL | 43.63 mL |
5 mM | 0.87 mL | 4.36 mL | 8.73 mL |
10 mM | 0.44 mL | 2.18 mL | 4.36 mL |
50 mM | 0.09 mL | 0.44 mL | 0.87 mL |
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References
References are publications that support the products' biological activity.
Pilotte et al (2012) Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc.Natl.Acad.Sci.U.S.A. 109 2497 PMID: 22308364
Dolusić et al (2011) Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. J.Med.Chem. 54 5320 PMID: 21726069
Keywords: LM 10, supplier, LM10, selective, 2,3-dioxygenase, TDO, inhibitors, inhibits, orally, bioavailable, anticancer, cancer, immunology, TDO, TDO, Tocris Bioscience