LM10

SKU: orb1222756

Description

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.

Key Properties

• CAS Number: 1316695-35-8
• MW: 229.22
• Purity: >98% (HPLC)
• Formula: C₁₁H₈FN₅
• SMILES: Fc2cc3ncc(/C=C/c1nnnn1)c3cc2
• Target: TDO
• Solubility: In Vitro: DMSO : 50 mg/mL (218.14 mM)

Bioactivity

• 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. 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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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LM10 | LM 10 | LM-10

Quick Database Links

Gene Symbol

TDO