BIBX 1382 96%

BIBX 1382

源叶(MedMol)
S80514
196612-93-8
C18H19ClFN7
387.8418
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S80514-5mg 96% ¥400.00元 6 - - -
源叶(MedMol) S80514-10mg 96% ¥690.00元 7 - - -
源叶(MedMol) S80514-25mg 96% ¥1180.00元 6 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

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
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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参考文献

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