| Bioactivity | 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]. | ||||||||||||
| Target | TDO | ||||||||||||
| 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: | ||||||||||||
| Name | LM10 | ||||||||||||
| CAS | 1316695-35-8 | ||||||||||||
| Formula | C11H8FN5 | ||||||||||||
| Molar Mass | 229.21 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |