Molecular Formula | C11H8FN5 |
Molar Mass | 229.21 |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
In vitro study | LM10 (Ki = 5.6 μm) had high selectivity and no inhibitory effect on IDO. |
In vivo study | LM10 had higher plasma concentrations and oral bioavailability after administration in mice. After oral administration of LM10 at 160 mg/kg/day to mice, the drug plasma concentration was between 20-40 μg/mL(87-175 μm). Systemic Treatment of immunized mice with LM10 at 160 (mg/kg)/day inhibited the growth of P815 tumor cells expressing TDO. LM10 treated mice showed no signs of toxicity |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.363 ml | 21.814 ml | 43.628 ml |
5 mM | 0.873 ml | 4.363 ml | 8.726 ml |
10 mM | 0.436 ml | 2.181 ml | 4.363 ml |
5 mM | 0.087 ml | 0.436 ml | 0.873 ml |
Biological activity | LM10 is a selective tryptophan dioxygenase (TDO) inhibitor. The IC50 for inhibiting human and mouse TDO is 0.62 μM and 2 μM respectively. |
target | TargetValue mTDO (in P815B cells) 2 μM |
Target | Value |
mTDO (in P815B cells) | 2 μM |
In vitro study | LM10 (Ki = 5.6 μM) has high selectivity and has no inhibitory effect on IDO. |
in vivo study | LM10 has high plasma concentration and oral bioavailability after administration in mice. After oral administration of 160 mg/kg/day LM10 in mice, the drug plasma concentration was between 20-40 μg/mL(87-175 μM). Systemic treatment of immunized mice with 160 (mg/kg)/day LM10 was able to inhibit the growth of P815 tumor cells expressing TDO. LM10 treated mice have no obvious toxic symptoms |