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LM10

Cat. No. M10116
LM10 Structure
Synonym:

LM-10

Size Price Availability Quantity
10mg USD 72  USD80 In stock
50mg USD 292.5  USD325 In stock
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Quality Control
Biological Activity

LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). LM10 exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. LM10 reduces growth of TDO-expressing P815 mastocytoma tumors in mice.

Protocol
Cell Experiment
Cell lines P815B cells
Preparation method 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).
Concentrations 2, 20, or 200 μM
Incubation time 8 h
Animal Experiment
Animal models DBA/2 mice
Formulation dissolved in water (1 mg/mL)
Dosages 160 mg/kg
Administration oral administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 229.21
Formula C11H8FN5
CAS Number 1316695-35-8
Purity 100.0%
Solubility DMSO ≥ 33 mg/mL
Storage at -20°C
References

Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase
Luc Pilotte, et al. Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502. PMID: 22308364.

Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators
Eduard Dolusic, et al. J Med Chem. 2011 Aug 11;54(15):5320-34. PMID: 21726069.

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Indoximod

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LM10, LM-10 supplier, IDO, inhibitors

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