CAS 1316695-35-8|LM10

Introduction:Basic information about CAS 1316695-35-8|LM10, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameLM10
CAS Number1316695-35-8Molecular Weight229.213
Density1.6±0.1 g/cm3Boiling Point522.5±60.0 °C at 760 mmHg
Molecular FormulaC11H8FN5Melting Point/
MSDS/Flash Point269.8±32.9 °C

Names

Name6-Fluoro-3-[(E)-2-(1H-tetrazol-5-yl)vinyl]-1H-indole
SynonymMore Synonyms

LM10 BiologicalActivity

DescriptionLM10 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 CatalogResearch Areas >>CancerSignaling Pathways >>Others >>Others
Target

TDO[1]

In VivoLM10 (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

[1]. Pilotte L, et al. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc Natl Acad Sci U S A. 2012;109(7):2497-2502.

Chemical & Physical Properties

Density1.6±0.1 g/cm3
Boiling Point522.5±60.0 °C at 760 mmHg
Molecular FormulaC11H8FN5
Molecular Weight229.213
Flash Point269.8±32.9 °C
Exact Mass229.076370
PSA70.25000
LogP1.80
Vapour Pressure0.0±1.4 mmHg at 25°C
Index of Refraction1.829
Storage condition-20℃

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
CAS 56880-88-7|4,5,5a,6,7,8-Hexahydro-1,5a-dimethyl-2H-2-benzazepine-3,9-dione
CAS 45807-05-4|1-(5-amino-1H-1,2,4-triazol-3-yl)guanidine
Recommended......
TOP