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.
|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 models||DBA/2 mice|
|Formulation||dissolved in water (1 mg/mL)|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 33 mg/mL|
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.
|Related IDO Products|
1-Methyl-L-tryptophan is an inhibitor of indoleamine 2,3-dioxygenase (IDO).
Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor.
Indoximod, also known as NLG8189 and D-1MT is an indoleamine 2,3-dioxygenase (IDO) pathway inhibitor with a Ki value of 19 μM.
IDO-IN-1 is a potent and selective indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM.
IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.