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Falnidamol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Falnidamol图片
CAS NO:196612-93-8
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
BIBX 1382
产品介绍
Falnidamol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。

产品描述

Falnidamol 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.

体外活性

Falnidamol displays >1000-fold lower potency against ErbB2 (IC50: 3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM) [1]. Falnidamol demonstrates antiproliferative activity in mitogenic assays performed with KB cells [2].

体内活性

Falnidamol (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 [2].

动物实验

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 [2].

Cas No.

196612-93-8

分子式

C18H19ClFN7

分子量

387.84

别名

BIBX 1382;Falnidamol

储存和溶解度

DMSO:28.8mg/mL (74.3mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years