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: 2025-08-27 01:20:12
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	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.

Precursor 3
1316695-32-5 399-51-9 2795-41-7
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