1316695-35-8
1316695-35-8 structure
- Name: LM10
- Chemical Name: 6-Fluoro-3-[(E)-2-(1H-tetrazol-5-yl)vinyl]-1H-indole
- CAS Number: 1316695-35-8
- Molecular Formula: C11H8FN5
- Molecular Weight: 229.213
- Catalog: Research Areas Cancer
- Create Date: 2018-12-25 10:34:33
- Modify Date: 2024-01-05 18:13:29
-
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].
| 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 | |
