Name | 6-Fluoro-3-[(E)-2-(1H-tetrazol-5-yl)vinyl]-1H-indole |
---|---|
Synonyms |
1H-Indole, 6-fluoro-3-[(E)-2-(1H-tetrazol-5-yl)ethenyl]-
6-Fluoro-3-[(E)-2-(1H-tetrazol-5-yl)vinyl]-1H-indole |
Description | LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO). Tryptophan 2,3-dioxygenase (TDO) is an unrelated hepatic enzyme that also degrades tryptophan along the kynurenine pathway. LM10 has the potential for the research of cancer diseases[1]. |
---|---|
Related Catalog | |
Target |
TDO[1] |
In Vivo | LM10 (160 mg/kg; p.o.) prevents the growth of TDO-expressing P815 tumor cells and promotes better rejection of control clone P815B cl1, which does not express TDO[1]. LM10 displays a good TDO inhibition (Ki = 5.6 μM) with a competitive inhibition profile[1]. LM10 does not inhibit IDO and has a high solubility and bioavailability without obvious signs of toxicity[1]. The plasma concentration of LM10 after oral administration of 160 mg/kg/day is between 20 and 40 μg/mL (87-175 μM), a concentration about 40 times above the IC50 measured in the cellular assay performed with the physiological concentration of plasma tryptophan[1]. Animal Model: DBA/2 mice (6-8 weeks)[1] Dosage: 160 mg/kg/day Administration: p.o. Result: Prevented the growth of TDO-expressing P815 tumor cells and promoted better rejection of control clone P815B cl1, which does not express TDO. |
References |
Density | 1.6±0.1 g/cm3 |
---|---|
Boiling Point | 522.5±60.0 °C at 760 mmHg |
Molecular Formula | C11H8FN5 |
Molecular Weight | 229.213 |
Flash Point | 269.8±32.9 °C |
Exact Mass | 229.076370 |
PSA | 70.25000 |
LogP | 1.80 |
Vapour Pressure | 0.0±1.4 mmHg at 25°C |
Index of Refraction | 1.829 |
Storage condition | -20℃ |
Precursor 3 | |
---|---|
DownStream 0 |