Nilotinib是一种口服可用的具有抗肿瘤活性的Bcr-Abl酪氨酸激酶抑制剂。
| 生物活性 | Nilotinib is an orally availableBcr-Abltyrosine kinase inhibitor with antineoplastic activity. |
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体外研究
(In Vitro) | Nilotinib (AMN107), selective Abl inhibitor, is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib while being significantly more potent compared with imatinib (IC50<30 nm), also maintains activity against most of the bcr-abl point mutants that confer imatinib resistance[1].
Nilotinib demonstrates significant antitumor efficacy against GIST xenograft lines and imatinib-resistant GIST cell lines which parent cell lines GK1C and GK3C shows imatinib sensitivity with IC50of 4.59±0.97 μM and 11.15±1.48 μM, respectively, imatinib-resistant cell lines GK1C-IR and GK3C-IR shows Imatinib resistance with IC50values of 11.74±0.17 μM (P<0.001) and 41.37±1.07 μM (P<0.001), respectively[2].
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体内研究
(In Vivo) | Nilotinib (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft[2].
Nilotinib has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model while decreases the PDGFR α and β levels and apoptotic scores in the colon[3].
| Animal Model: | BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)[2] | | Dosage: | 40 mg/kg | | Administration: | Oral gavage; daily; 4 weeks | | Result: | Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line. |
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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 : 12.5 mg/mL(23.61 mM;ultrasonic and warming and heat to 60℃) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液 | 1 mM | 1.8885 mL | 9.4425 mL | 18.8850 mL | | 5 mM | 0.3777 mL | 1.8885 mL | 3.7770 mL | | 10 mM | 0.1889 mL | 0.9443 mL | 1.8885 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： 10% DMSO 90%corn oil Solubility: ≥ 0.5 mg/mL (0.94 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (0.94 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 5.0 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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