FALNIDAMOL
| 中文名称 | FALNIDAMOL |
|---|---|
| 中文同义词 | 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;化合物BIBX 1382;BIBX1382游离态;N4-(3-氯-4-氟-苯基)-N6-(1-甲基-4-哌啶)嘧啶并5,4-D嘧啶-4,6-二胺;化合物FALNIDAMOL;N8-(3-氯-4-氟苯基)-N2-(1-甲基哌啶-4-基)嘧啶并[5,4-D]嘧啶-2,8-二胺;化合物FALNIDAMOL,10 MM DMSO 溶液;BIBX 1382【CAS：196612-93-8】【规格：50mg】【纯度：≥97%】 |
| 英文名称 | Bibx 1382 dihydrochloride |
| 英文同义词 | 8-(3-Chloro-4-fluoroanilino)-2-((1-methyl-4-piperidyl)amino)pyrimido(5,4-D)pyrimidine;Falnidamol;Falnidamol [inn];Pyrimido(5,4-D)pyrimidine-2,8-diamine, N8-(3-chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-;Unii-0mu316797d;N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diaminedihydrochloride;Falnid;N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-2,8-diamine |
| CAS号 | 196612-93-8 |
| 分子式 | C18H19ClFN7 |
| 分子量 | 387.84 |
| EINECS号 | |
| 相关类别 | 实验化学品 |
| Mol文件 | 196612-93-8.mol |
| 结构式 |  |
FALNIDAMOL 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） |
| 形态 | 固体 |
| 酸度系数(pKa) | 8+-.0.10(Predicted) |
| 颜色 | 淡黄色至黄色凝胶至 |
| 水溶解性 | water: 1mg/mL DMSO: 25mg/mL |
| InChI | 1S/C18H19ClFN7/c1-27-6-4-11(5-7-27)25-18-21-9-15-16(26-18)17(23-10-22-15)24-12-2-3-14(20)13(19)8-12/h2-3,8-11H,4-7H2,1H3,(H,21,25,26)(H,22,23,24) |
| InChIKey | FTFRZXFNZVCRSK-UHFFFAOYSA-N |
| SMILES | Fc1c(cc(cc1)Nc2ncnc3c2nc(nc3)NC4CCN(CC4)C)Cl |
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。
|
EGFR 3 nM (IC 50 ) |
ErbB2 3.4 μM (IC 50 ) |
Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.
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. |
安全信息
| WGK Germany | WGK 2 |
|---|---|
| 存储类别 | 11 - 可燃固体 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/09/15 | HY-10322R | FALNIDAMOL Falnidamol (Standard) | 196612-93-8 | 1 mg | 820元 |
| 2026/09/15 | HY-10322R | FALNIDAMOL Falnidamol (Standard) | 196612-93-8 | 5 mg | 2050元 |