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• 产品描述： Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity

• 靶点： EGFR:3 nM (IC50);ErbB2:3.4 μM (IC50);EGFR

• 体外研究：
  Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells

• 体内研究：
  Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment. Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice. With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM. Animal Model: Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells Dosage: 10 mg/kg Administration: p.o.; daily; 16 days Result: Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment. Animal Model: Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: p.o.; daily; 16 days Result: The C4h is 2222 nM and the C24h is 244 nM.

• 参考文献：
  1. Dittrich Ch, et al. Phase I and pharmacokinetic study of BIBX 1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur J Cancer. 2002 May;38(8):1072-80. 2. Solca FF, et al. Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J Pharmacol Exp Ther. 2004 Nov;311(2):502-9.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.578 ml	12.892 ml	25.784 ml
  5 mM	0.516 ml	2.578 ml	5.157 ml
  10 mM	0.258 ml	1.289 ml	2.578 ml
  50 mM	0.052 ml	0.258 ml	0.516 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 *