Gefitinib dihydrochloride(Synonyms: ZD 1839 dihydrochloride)

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Gefitinib dihydrochloride (Synonyms: ZD 1839 dihydrochloride)

Gefitinib dihydrochloride (ZD 1839 dihydrochloride) 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 dihydrochloride 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 dihydrochloride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。

Gefitinib dihydrochloride(Synonyms: ZD 1839 dihydrochloride)

Gefitinib dihydrochloride Chemical Structure

CAS No. : 184475-56-7

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Gefitinib dihydrochloride 的其他形式现货产品:

Gefitinib

生物活性

Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer [1][2][5].

IC50 & Target

IC50: 37 nM (Tyr1173 site, in NR6wtEGFR cells), 37 nM (Tyr992 site, in NR6wtEGFR cells)[1].
体外研究
(In Vitro)

Gefitinib dihydrochloride (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 dihydrochloride (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth[2].
Gefitinib dihydrochloride (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 dihydrochloride (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration[3].
Gefitinib dihydrochloride (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells)[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 dihydrochloride (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model[3].
Gefitinib dihydrochloride (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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

519.82

Formula

C22H26Cl3FN4O3
CAS 号

184475-56-7
中文名称

吉非替尼二盐酸盐
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wakeling AE, et al. ZD1839: an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54.

    [2]. Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23.

    [3]. Muhammad Tariq, et al. Gefitinib inhibits M2-like polarization of tumor-associated macrophages in Lewis lung cancer by targeting the STAT6 signaling pathway. Acta Pharmacol Sin. 2017 Nov;38(11):1501-1511.

    [4]. Mark S Cragg, et al. Gefitinib-induced killing of NSCLC cell lines expressing mutant EGFR requires BIM and can be enhanced by BH3 mimetics. PLoS Med. 2007 Oct;4(10):1681-89; discussion 1690.

    [5]. Marie P Piechocki, et al. Gefitinib prevents cancer progression in mice expressing the activated rat HER2/neu. Int J Cancer. 2008 Apr 15;122(8):1722-9.

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