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

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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
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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

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