Epacadostat (INCB024360) analogue

製品コードS7587 バッチS758705

印刷

化学情報

Chemical Structure Synonyms INCB14943 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C9H7ClFN5O2
分子量 271.64 CAS No. 914471-09-3
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 54 mg/mL (198.79 mM)
Ethanol (warmed with 50ºC water bath) 54 mg/mL (198.79 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 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 Epacadostat (INCB024360) analogue (INCB14943) is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Phase 2.
in vitro

In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 nM. [1] In coculture systems of human allogeneic lymphocytes with dendritic cells or tumor cells, INCB024360, via IDO1 inhibition, reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs, and increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells. [2]
in vivo

In mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. [1] INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice. [2]

プロトコル(参考用のみ)

キナーゼアッセイ IDO enzyme assays
Human IDO with an N-terminal His tag is expressed in E.coli and purified to homogeneity. IDO catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays are performed at room temperature using 20 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 3.5 μM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates are recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine.
動物実験 動物モデル Mice bearing GM-CSF-secreting B16 tumors
投薬量 75 mg/kg b.i.d
投与方法 s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/19507862/
  • https://pubmed.ncbi.nlm.nih.gov/20197554/

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：

IDO1 inhibitors are synergistic with CXCL10 agonists in inhibiting colon cancer growth [ Biomed Pharmacother, 2024, 179:117412] PubMed: 39255734
Granulocytic myeloid-derived suppressor cells increase infection risk via the IDO/IL-10 pathway in patients with hepatitis B virus-related liver failure [ Front Immunol, 2022, 13:966514] PubMed: 36685516
[ Oncoimmunology, 2017, ] PubMed: 29209565

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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