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• 产品描述： Itacitinib (INCB39110)是Janus-associated kinase 1 (JAK1)的抑制剂，具有口服生物活性和潜在的抗肿瘤活性

• 靶点： JAK1;JAK

• 体外研究：
  INCB039110是有效的、选择性的JAK1抑制剂，对JAK1的选择性分别是对JAK2和JAK3的20和200倍以上。对JAK1、2、3和TYK2的活性分别为2, 63, >2000 和 795 nM

• 体内研究：
  使用临床剂量的INCB039110，无论是其单药给药还是和毒性药剂如gemcitabine组合给药，可在携有胰腺异种移植瘤的小鼠中阻止肿瘤的生长

• 细胞实验： Cell lines: Monocyte-Derived Macrophages Concentrations: 1 μM Incubation Time: 1 h Method: Cells were treated with various concentrations of Itacitinib.

• 动物实验： Animal Models: Male Sprague-Dawley rats Dosages: 30 mg/kg Administration: s.c.

• 参考文献：
  1. Kettle JG, et al. Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1. Expert Opin Ther Pat. 2017, 27(2):127-143 2. Jun Li, et al. Abstract 779: Blockade of the IL-6/JAK/STAT3 signaling pathway inhibits pancreatic tumor cell growth in 3D spheroid cultures and in xenograft models . AACR; Cancer Res. 2015, 75(15 Suppl):Abstract nr 779. 3. Lescoat A, et al. Combined anti-fibrotic and anti-inflammatory properties of JAK-inhibitors on macrophages in vitro and in vivo: Perspectives for scleroderma-associated interstitial lung disease. Biochem Pharmacol. 2020 Aug;178:114103. 4. Chen Y, et al. Zhuye Shigao Decoction Combined with Qingqi Huatan Pills in Alleviating the Acute Exacerbation of Chronic Obstructive Pulmonary Disease (Phlegm-Heat Stagnating in the Lungs) via the IL-6-Mediated JAK1/STAT3 Signaling Pathway. Evid Based Complement Alternat Med. 2022 May 6;2022:7942623.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.807 ml	9.033 ml	18.066 ml
  5 mM	0.361 ml	1.807 ml	3.613 ml
  10 mM	0.181 ml	0.903 ml	1.807 ml
  50 mM	0.036 ml	0.181 ml	0.361 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *