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 |
|
注意: |
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