• 提示：详情请下载说明书。

• 产品描述： Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity

• 靶点： FGFR4:1.9 nM (IC50);FGFR1:>10 μM (IC50);FGFR2:>10 μM (IC50);FGFR3:>10 μM (IC50);rat FGFR4:>10 μM (IC50);FGFR

• 体外研究：
  Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (IC50= 1.9 nM). Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC50>10 uM). Roblitinib inhibits HUH7 (IC50=12 nM), Hep3B (IC50=9 nM), JHH7 (IC50=9 nM), HEPG2 (IC50>10 uM), JHH (IC50>10 uM)

• 体内研究：
  Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model. Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days. Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a Vss of 2.3 L/kg for Male mice (C57BL/6) . Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2 of 4.4 hours, a CL of 19 mL/min•kg, and a Vss of 3.9 L/kg for male SD rats. Animal Model: Male Wistar Hannover rats (Hep3B xenograft model) Dosage: 10, 30, 100 mg/kg Administration: Gavage; for 10 days Result: Caused blood concentrations dropped below the IC90 threshold between 8 and 12 h following dosing.Had the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model. Animal Model: Male mice (C57BL/6) Dosage: 1 mg/kg or 3 mg/kg (Pharmacokinetic Analysis) Administration: IV at 1 mg/kg; PO at 3 mg/kg Result: Had a T1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a Vss of 2.3 L/kg.

• 参考文献：
  1. Nicole Buschmann, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. WO2015059668A1. 2. Robin A Fairhurst, et al. Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. J Med Chem. 2020 Nov 12;63(21):12542-12573.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.974 ml	9.871 ml	19.741 ml
  5 mM	0.395 ml	1.974 ml	3.948 ml
  10 mM	0.197 ml	0.987 ml	1.974 ml
  50 mM	0.039 ml	0.197 ml	0.395 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

输入产品批号：

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 *