Home Metabolism IDO/TDO inhibitor LM10 For research use only.

LM10

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.

LM10 Chemical Structure

LM10 Chemical Structure

CAS: 1316695-35-8

Selleck's LM10 has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.32%
99.32

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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
In vitro LM10 (Ki=5.6 μM) displays an excellent selectively prolfile and does not display any inhibitory potency on IDO[1].
Cell Research 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).
In Vivo
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].
Animal Research Animal Models DBA/2 mice
Dosages 160 mg/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02315183 Completed
Acute Kidney Injury
University of Leicester
 January 2014 --

Chemical Information & Solubility

Molecular Weight 229.21 Formula

C11H8FN5
CAS No. 1316695-35-8 SDF Download LM10 SDF
Smiles C1=CC2=C(C=C1F)NC=C2C=CC3=NNN=N3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 46 mg/mL ( (200.68 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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