Falnidamol (BIBX 1382) 是一种具有口服活性的，选择性的EGFR 酪氨酸激酶抑制剂，IC50为3 nM。Falnidamol 对 ErbB2 (IC50=3.4 μM) 和其他一系列相关酪氨酸激酶 (IC50>10 μM) 的选择性 >1000倍。Falnidamol 是嘧啶-嘧啶化合物，具有抗癌活性。
| 生物活性 | Falnidamol (BIBX 1382) is an orally active, selectiveEGFRtyrosine kinaseinhibitor with anIC50of 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]. |
| IC50& Target[1] | EGFR 3 nM (IC50) | ErbB2 3.4 μM (IC50) |
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体外研究
(In Vitro) | Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells[2].
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体内研究
(In Vivo) | 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 C4his 2222 nM and the C24his 244 nM[2].
| Animal Model: | Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells[2] | | 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[2] | | Dosage: | 10 mg/kg (Pharmacokinetic Analysis) | | Administration: | p.o.; daily; 16 days | | Result: | The C4his 2222 nM and the C24his 244 nM. |
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| Clinical Trial | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 31.25 mg/mL(80.57 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.5784 mL | 12.8919 mL | 25.7838 mL | | 5 mM | 0.5157 mL | 2.5784 mL | 5.1568 mL | | 10 mM | 0.2578 mL | 1.2892 mL | 2.5784 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 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。 *以上所有助溶剂都可在本网站选购。
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