ChemicalBook CAS数据库列表 FALNIDAMOL
FALNIDAMOL
- CAS号:196612-93-8
- 英文名:BIBX 1382 DIHYDROCHLORIDE
- 中文名:FALNIDAMOL
- CBNumber:CB6842590
- 分子式:C18H19ClFN7
- 分子量:387.84
- MOL File:196612-93-8.mol
FALNIDAMOL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 :DMSO (Slightly), Methanol (Slightly)
- 酸度系数(pKa) :8?+-.0.10(Predicted)
- 形态 :Solid
- 颜色 :Pale Yellow to Yellow
FALNIDAMOL性质、用途与生产工艺
- 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。
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靶点
EGFR
3 nM (IC 50 )
ErbB2
3.4 μM (IC 50 )
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体外研究
Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.
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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.
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FALNIDAMOL 试剂级价格
- 更新日期：2024/11/08
- 产品编号：HY-10322
- 产品名称：Falnidamol
- CAS编号：
- 包装：1 mg
- 价格：350元
- 更新日期：2024/11/08
- 产品编号：HY-10322
- 产品名称：FALNIDAMOL Falnidamol
- CAS编号：196612-93-8
- 包装：5mg
- 价格：820元
FALNIDAMOL生产厂家
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
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