LM10

製品コードS8368 バッチS836803

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C11H8FN5
分子量 229.21 CAS No. 1316695-35-8
Solubility (25°C)* 体外 DMSO 46 mg/mL (200.68 mM)
Ethanol 20 mg/mL (87.25 mM)
Water ˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50 values of 0.62 and 2 μM for human and mouse TDO, respectively.
in vitro LM10 (Ki=5.6 μM) displays an excellent selectively prolfile and does not display any inhibitory potency on IDO[1].
in vivo LM10 has high plasma concentration and oral bioavailability in mouse. 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. Systemic treatment of immunized mice with LM10 at 160 (mg/kg)/day prevents the growth of TDO-expressing P815 tumor cells. Moreover, mice treated with LM10 do not show obvious signs of toxicity[1][2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 P815B cells
濃度 2, 20, or 200 μM
反応時間 8 h
実験の流れ The assay is performed in 96-well flat bottom plates seeded with 2×105 cells in a final volume of 200 μL. 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).
動物実験 動物モデル DBA/2 mice
投薬量 160 mg/kg
投与方法 oral administration

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Tumor-associated nonmyelinating Schwann cell-expressed PVT1 promotes pancreatic cancer kynurenine pathway and tumor immune exclusion [ Sci Adv, 2023, 9(5):eadd6995] PubMed: 36724291
Tryptophan 2, 3‑dioxygenase promotes proliferation, migration and invasion of ovarian cancer cells [ Mol Med Rep, 2021, 23(6)445] PubMed: 33846800
Tryptophan 2,3-dioxygenase inhibitory activities of tryptanthrin derivatives [Zhang S, et al. Eur J Med Chem, 2018, 160:133-145] PubMed: 30321802

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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