貨號	規格	價格	上海	北京	武漢	南京
S80514-5mg	99.1%	￥400.00 S80514-5mg ￥400.00 現貨	6 6	-	-	-
S80514-10mg	99.1%	￥690.00 S80514-10mg ￥690.00 現貨	7 7	-	-	-
S80514-25mg	99.1%	￥1180.00 S80514-25mg ￥1180.00 現貨	6 6	-	-	-

產品介紹

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

產品描述：

靶點：

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

體外研究：

Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells

體內研究：

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.

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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