196612-93-8
中文名称
FALNIDAMOL
英文名称
BIBX 1382 DIHYDROCHLORIDE
CAS
196612-93-8
分子式
C18H19ClFN7
分子量
387.84
MOL 文件
196612-93-8.mol
更新日期
2024/06/17 17:25:41
196612-93-8 结构式
基本信息
中文别名
N8-(3-氯-4-氟苯基)-N2-(1-甲基-4-哌啶基)嘧啶并[5,4-D]嘧啶-2,8-二胺 英文别名
FalnidCS-928
Falnidamol
Unii-0mu316797d
Falnidamol [inn]
BIBX 1382 DIHYDROCHLORIDE
FALNIDAMOL
BIBX-1382
BIBX 1382
8-(3-Chloro-4-fluoroanilino)-2-((1-methyl-4-piperidyl)amino)pyrimido(5,4-D)pyrimidine
N4-(3-chloro-4-fluoro-phenyl)-N6-(1-methyl-4-piperidyl)pyrimido[5,4-d]pyrimidine-4,6-diamine
N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-2,8-diamine
物理化学性质
熔点>217°C (dec.)
沸点552.0±60.0 °C(Predicted)
密度1.427
储存条件Keep in dark place,Inert atmosphere,2-8°C
溶解度可溶于DMSO（少许）、甲醇（少许）
酸度系数(pKa)8?+-.0.10(Predicted)
形态固体
颜色淡黄色至黄色
常见问题列表
生物活性
Falnidamol (BIBX 1382) 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。靶点
|
EGFR 3 nM (IC 50 ) |
ErbB2 3.4 μM (IC 50 ) |
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 C
4h
is 2222 nM and the C
24h
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 C 4h is 2222 nM and the C 24h is 244 nM. |