Falnidamol (BIBX 1382) 是一种具有口服

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^[1][2].

Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells^[2]. 

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^[2]. 
Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice^[2]. 
With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C_4h is 2222 nM and the C_24h is 244 nM^[2]. 

387.84

Solid

C₁₈H₁₉ClFN₇

196612-93-8

Room temperature in continental US; may vary elsewhere.

DMSO : 31.25 mg/mL (80.57 mM; ultrasonic and warming and heat to 60°C)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 2 years; -20℃, 1 year。-80℃ 储存时，请在 2 年内使用， -20℃ 储存时，请在 1 年 内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 1.67 mg/mL (4.31 mM); Clear solution

   

  此方案可获得 ≥ 1.67 mg/mL (4.31 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

• [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.  [Content Brief]

  [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.  [Content Brief]