196612-93-8
中文名稱
FALNIDAMOL
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
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 英文別名
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
物理化學(xué)性質(zhì)
熔點(diǎn)>217°C (dec.)
沸點(diǎn)552.0±60.0 °C(Predicted)
密度1.427
儲(chǔ)存條件Keep in dark place,Inert atmosphere,2-8°C
溶解度可溶于DMSO（少許）、甲醇（少許）
酸度系數(shù)(pKa)8?+-.0.10(Predicted)
形態(tài)固體
顏色淡黃色至黃色
常見(jiàn)問(wèn)題列表
生物活性
Falnidamol (BIBX 1382) 是一種具有口服活性的，選擇性的 EGFR 酪氨酸激酶抑制劑，IC50 為3 nM。Falnidamol 對(duì) ErbB2 (IC50=3.4 μM) 和其他一系列相關(guān)酪氨酸激酶 (IC50>10 μM) 的選擇性 >1000倍。Falnidamol 是嘧啶-嘧啶化合物，具有抗癌活性。靶點(diǎn)
|
EGFR 3 nM (IC 50 ) |
ErbB2 3.4 μM (IC 50 ) |
體外研究
Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.
體內(nèi)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. |