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