LM10

Catalog No.S8368

LM10 Chemical Structure

Molecular Weight(MW): 229.21

LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50 values of 0.62 and 2 μM for human and mouse TDO, respectively.

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Biological Activity

Description LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50 values of 0.62 and 2 μM for human and mouse TDO, respectively.
Targets
mTDO [1]
(in P815B cells)
2 μM
In vitro

LM10 (Ki=5.6 μM) displays an excellent selectively prolfile and does not display any inhibitory potency on IDO[1].

In vivo LM10 has high plasma concentration and oral bioavailability in mouse. 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. Systemic treatment of immunized mice with LM10 at 160 (mg/kg)/day prevents the growth of TDO-expressing P815 tumor cells. Moreover, mice treated with LM10 do not show obvious signs of toxicity[1][2].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: P815B cells
  • Concentrations: 2, 20, or 200 μM
  • Incubation Time: 8 h
  • Method: The assay is performed in 96-well flat bottom plates seeded with 2×105 cells in a final volume of 200 μL. To determine the TDO inhibitory potency of the synthesized molecules, the cells are incubated for 8 h at 37℃ in HBSS (Hanks' balanced salt solution), supplemented with 80 μM L-tryptophan and 2, 20, or 200 μM of the studied compound. To determine the IC50, the cells are incubated for 8 h at 37℃ in HBSS supplemented with 80 μM L-tryptophan and a titration of the compound ranging from 0.3 to 80 μM or from 1.5 to 400 μM. The plates are then centrifuged for 10 min at 300g, and 150 μL of the supernatant is collected. The wells are preserved for cell viability evaluation. The supernatant is analyzed by HPLC to measure the concentration of residual tryptophan and produced kynurenine, based on the retention time and the UV absorption (280 nm for tryptophan, 360 nm for kynurenine).
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: DBA/2 mice
  • Formulation: Drinking water
  • Dosages: 160 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 45 mg/mL (196.32 mM)
Ethanol 11 mg/mL (47.99 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 229.21
Formula

C11H8FN5

CAS No. 1316695-35-8
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID