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编 号:F118719
分子式:C11H8FN5
分子量:229.21
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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生物活性:
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.

体内研究:
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. LM10 displays a good TDO inhibition (Ki = 5.6 μM) with a competitive inhibition profile.LM10 does not inhibit IDO and has a high solubility and bioavailability without obvious signs of toxicity.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.Animal Model:DBA/2 mice (6-8 weeks)
Dosage:160 mg/kg/day
Administration:p.o.
Result:Prevented the growth of TDO-expressing P815 tumor cells and promoted better rejection of control clone P815B cl1, which does not express TDO.
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