LM10

Modify Date: 2024-01-05 18:13:29

LM10 structure	Common Name	LM10
	CAS Number	1316695-35-8	Molecular Weight	229.213
	Density	1.6±0.1 g/cm3	Boiling Point	522.5±60.0 °C at 760 mmHg
	Molecular Formula	C₁₁H₈FN₅	Melting Point	N/A
	MSDS	N/A	Flash Point	269.8±32.9 °C

Use of LM10

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
Synonym	More Synonyms

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	Research Areas >> Cancer Signaling Pathways >> Others >> Others
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	[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.

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℃