Lapatinib (GW572016) 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。
| 生物活性 | Lapatinib (GW572016) is a potent inhibitor of theErbB-2andEGFRtyrosine kinase domains withIC50values against purifiedEGFRandErbB-2of 10.2 and 9.8 nM, respectively[1]. |
| IC50& Target | EGFR 10.2 nM (IC50, Cell Free Assay) | ErbB2 9.8 nM (IC50, Cell Free Assay) |
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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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(215.12 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7210 mL | 8.6050 mL | 17.2099 mL | | 5 mM | 0.3442 mL | 1.7210 mL | 3.4420 mL | | 10 mM | 0.1721 mL | 0.8605 mL | 1.7210 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： 12%SBE-beta-CD Solubility: 5 mg/mL (8.60 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂： 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (4.30 mM); Suspended solution; Need ultrasonic 3. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.58 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 4. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (3.58 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (3.58 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 5. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.58 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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