Falnidamol(Synonyms: BIBX 1382)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Falnidamol (Synonyms: BIBX 1382) 纯度: 96.25%

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。

Falnidamol(Synonyms: BIBX 1382)

Falnidamol Chemical Structure

CAS No. : 196612-93-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1089 In-stock
5 mg ￥990 In-stock
10 mg ￥1760 In-stock
50 mg ￥6050 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Falnidamol 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Differentiation Inducing Compound Library
  • Orally Active Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Falnidamol (BIBX 1382) 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[1][2].

IC50 & Target[1]

EGFR

3 nM (IC50)

ErbB2

3.4 μM (IC50)

体外研究
(In Vitro)

Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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[2].
Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice[2].
With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells[2]
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[2]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: p.o.; daily; 16 days
Result: The C4h is 2222 nM and the C24h is 244 nM.

Clinical Trial

分子量

387.84

Formula

C18H19ClFN7
CAS 号

196612-93-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 41 mg/mL (105.71 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5784 mL 12.8919 mL 25.7838 mL
5 mM 0.5157 mL 2.5784 mL 5.1568 mL
10 mM 0.2578 mL 1.2892 mL 2.5784 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (4.31 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (4.31 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Dittrich Ch, et al. Phase I and pharmacokinetic study of BIBX 1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur J Cancer. 2002 May;38(8):1072-80.

    [2]. Solca FF, et al. Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J Pharmacol Exp Ther. 2004 Nov;311(2):502-9.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务