Lapatinib ditosylate(Synonyms: 二甲苯磺酸拉帕替尼; GW572016 ditosylate; GW2016 ditosylate)

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。

Lapatinib ditosylate (Synonyms: 二甲苯磺酸拉帕替尼; GW572016 ditosylate; GW2016 ditosylate) 纯度: 99.95%

Lapatinib ditosylate (GW572016 ditosylate) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC50 值分别为 10.2 和 9.8 nM。

Lapatinib ditosylate(Synonyms: 二甲苯磺酸拉帕替尼; GW572016 ditosylate; GW2016 ditosylate)

Lapatinib ditosylate Chemical Structure

CAS No. : 388082-77-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥770 In-stock
50 mg ￥700 In-stock
100 mg ￥1200 In-stock
500 mg ￥3000 In-stock
1 g ￥4500 In-stock
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

Lapatinib ditosylate 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Ferroptosis Compound Library
  • Anti-COVID-19 Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug 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
  • Targeted Therapy Drug Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].

IC50 & Target

EGFR

10.8 nM (IC50, Cell Free Assay)

ErbB2

9.2 nM (IC50, Cell Free Assay)

体外研究
(In Vitro)

Lapatinib (GW2016; 0.03-10 µM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner[1].
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines[1].
Lapatinib (GW2016; 1-10 µM; 72 hours; HN5 cells) treatment results in induces G1 arrest[1].

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.

Western Blot Analysis[1]

Cell Line: BT474 and HN5 cells
Concentration: 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM
Incubation Time: 6 hours
Result: Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: HN5, A-43, BT474, N87, and CaLu-3 cells
Concentration:
Incubation Time: 72 hours
Result: Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

Cell Cycle Analysis[1]

Cell Line: HN5 cells
Concentration: 1 µM, or 10 µM
Incubation Time: 72 hours
Result: Resulted in induction of G1 arrest.

体内研究
(In Vivo)

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose[1].

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: CD-1 nude female mice (4-6 weeks old) with HN5 cells[1]
Dosage: 30 mg/kg, 100 mg/kg
Administration: Oral administration; twice daily; for 21 days
Result: Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

Clinical Trial

分子量

925.46

Formula

C43H42ClFN4O10S3
CAS 号

388082-77-7
中文名称

二甲苯磺酸拉帕替尼；二对甲苯磺酸拉帕替尼；拉帕替尼泊
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (135.07 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0805 mL 5.4027 mL 10.8054 mL
5 mM 0.2161 mL 1.0805 mL 2.1611 mL
10 mM 0.1081 mL 0.5403 mL 1.0805 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 (sealed storage, away from moisture and light)。-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: ≥ 2.33 mg/mL (2.52 mM); Clear solution

    此方案可获得 ≥ 2.33 mg/mL (2.52 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 23.3 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

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.33 mg/mL (2.52 mM); Clear solution

    此方案可获得 ≥ 2.33 mg/mL (2.52 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 23.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*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]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94

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

发表回复