Gefitinib (ZD1839) 是一种有效，选择性和口服活性的EGFR酪氨酸激酶抑制剂，IC50为 33 nM。Gefitinib 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC50为 54 nM)，并阻断 EGF 刺激的肿瘤细胞中EGFR自磷酸化。Gefitinib 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)，可用于癌症相关的研究，如肺癌和乳腺癌。
| 生物活性 | Gefitinib (ZD1839) is a potent, selective and orally activeEGFRtyrosine kinaseinhibitor with anIC50of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50of 54 nM) and that blocks EGF-stimulatedEGFRautophosphorylation in tumor cells. Gefitinib also inducesautophagyand cellapoptosis, which can be used forcancerrelated research, such as Lungcancerand breastcancer[1][2][5]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Gefitinib (0.01-0.1 μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth[2].
Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth[2].
Gefitinib (0.62 μM, 24-72 h) inhibits IL-13-induced M2-like polarization of RAW 264.7 cells through the STAT6-dependent signaling pathway[3].
Gefitinib (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration[3].
Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells)[4].
Gefitinib (100 nM, 24 h) suppresses macropinocytosis and increases the cellular uptake of extracellular vesicles( EVs) in HCC827 and A549 cells[6].
Gefitinib (1.5-60 μM, 48 h) increases inhibition of proliferation in H358Rand A549Rcells (Cisplatin-resistant wtEGFR NSCLC cell lines)[7].
Western Blot Analysis[2] | Cell Line: | NR6wtEGFR, NR6W and NR6M | | Concentration: | 1, 10, 100 μM | | Incubation Time: | 5 h | | Result: | Inhibited EGFR tyrosine phosphorylations. |
Cell Migration Assay[3] | Cell Line: | LLCs cell | | Concentration: | 0.62 μM | | Incubation Time: | 72 h | | Result: | Abrogated M2-like macrophage promoted invasion and migration of LLCs. |
|
体内研究
(In Vivo) | Gefitinib (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model[3].Gefitinib (Oral administration, 75 mg/kg for the initial week, daily for 5 consecutive days per week) eliminates phosphorylation of HER2 and HER3 and signaling through MAPK and Akt in lobular hyperplasias and carcinomas, increases MAPK activity and cytokine production in splenocytes and lymph nodes[5].
Gefitinib (Oral gavage, 150 mg/kg, daily) enhances the anti-tumor effect of Cisplatin in H358Rxenograft[7].
| Animal Model: | LLC mice metastasis model[3] | | Dosage: | 75 mg/kg/d, for 21 days. | | Administration: | Oral administration | | Result: | Reduced the number of lung metastasis nodules, down-regulated the expression of M2 marker genes and the percentages CD206+and CD68+macrophages in tumor tissues. |
| Animal Model: | BALB-NeuT transgenic mouse model[5] | | Dosage: | 75 mg/kg for the initial week, and increased by 15 mg/kg every other week, daily for 5 consecutive days per week, followed by 2 days without treatment and repeated for 8–9 weeks. | | Administration: | Oral administration | | Result: | Reduced tumor multiplicity from 9.6 to 0.58 (83%), and reduced the number and size of lobules and lobular nodules in treated mice. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 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 : 125 mg/mL(279.70 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2376 mL | 11.1882 mL | 22.3764 mL | | 5 mM | 0.4475 mL | 2.2376 mL | 4.4753 mL | | 10 mM | 0.2238 mL | 1.1188 mL | 2.2376 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: ≥ 2.5 mg/mL (5.59 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.59 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.65 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.65 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 1% DMSO 99% saline Solubility: 0.5 mg/mL (1.12 mM); Suspended solution; Need ultrasonic *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com