Gefitinib

产品编号 T1181   CAS 184475-35-2
别名: 吉非替尼, ZD1839

Gefitinib is an EGFR tyrosine kinase inhibitor and can inhibit Tyr1173, Tyr992, Tyr1173 and Tyr992 (IC50s: 37/37/26/57 nM).

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Gefitinib结构式
Gefitinib , CAS 184475-35-2
规格 库存 价格/RMB 数量
100 mg 上海现货 525.00
500 mg 上海现货 885.00
1 g 上海现货 1290.00
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纯度 100.00%
纯度 99.92%
纯度 98.00%
纯度 100.00%
纯度 100.00%
纯度 100.00%
纯度 100.00%
生物活性
化学信息
存储 & 溶解度
配制溶液
产品描述 Gefitinib is an EGFR tyrosine kinase inhibitor and can inhibit Tyr1173, Tyr992, Tyr1173 and Tyr992 (IC50s: 37/37/26/57 nM).
靶点活性 Tyr1173 (NR6W cells)   Tyr1173 (NR6wtEGFR cells)   Tyr992 (NR6W cells)   Tyr992 (NR6wtEGFR cells)   Tyr1173   Tyr992
体外活性 Gefitinib (0.001–2 μM) effectively inhibited all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines. The calculated IC50 values for these sites were 37 nM (Tyr1173), 37 nM (Tyr992), 26 nM (Tyr1173) and 57 nM (Tyr992) in, respectively, the low and high EGFR expressing cell lines. As opposed to the level of ERK phosphorylation the high EGFR-expressing cell line had a substantial level of PLC-γ phosphorylation after EGF stimulation as compared to the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib effectively blocked this phosphorylation (IC50: 27 nM). The NR6wtEGFR and NR6M cell lines had low levels of PLC-γ phosphorylations but the level in the NR6M cell line was more resistant to inhibition by gefitinib (IC50: 43/369 nM) [1]. Treatment with gefitinib alone lead to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC50 of 2 μmol/L. H1299, H460, H1975, CALU-3 GEF-R, and A549 cancer cell lines showed a limited sensitivity to gefitinib treatment with about 80% to 90% cells surviving at 5 μmol/L dose of EGFR inhibitor [2]. Gefitinib (0.5 μM, incubated days 1–5) significantly increased the anti-proliferative effect of fractionated radiation treatment (2 Gy day−1, days 1–3) on LoVo cells grown in vitro [3].
体内活性 Treatment with metformin or gefitinib (150 mg/kg daily orally by gavage), as single agents, caused a slight decrease in tumor size as compared with control untreated mice. Treatment with the combination of metformin and gefitinib induced a significant reduction in tumor growth [2]. The response of the LoVo xenografts to 5 Gy plus ZD1839 (100 mg/kg) was significantly enhanced compared with that seen with either drug or radiotherapy alone [3]. Compared with that in the control group, metastatic tumor burden did not increase after the start of gefitinib treatment, and the average bioluminescence value of tumors in the gefitinib treatment group was 24 × 10^6 photons/s on the final day of the study [4].
细胞实验 The human NSCLC H1299, H1975, A549, H460, GLC82, H460, and CALU-3 cell lines were provided by the American Type Culture Collection and maintained in RPMI-1640 supplemented with 10% FBS in a humidified atmosphere with 5% CO2. CALU-3 GEF-R is a cell line obtained in vitro as previously described. Briefly, over a period of 12 months, human CALU-3 lung adenocarcinoma cells were continuously exposed to increasing concentrations of gefitinib. The starting dose was the dose causing the inhibition of 50% of cancer cell growth (IC50; gefitinib, 1 μmol/L). The drug dose was progressively increased to 15 μmol/L in approximately 2 months, to 20 μmol/L after other 2 months, to 25 μmol/L after additional 2 months, and, finally, to 30 μmol/L for a total of 12 months. The established resistant cancer cell lines were then maintained in continuous culture with the maximally achieved dose of each TKI that allowed cellular proliferation (30 μmol/L for each drug) [2]. Cell lines: NR6, NR6M and NR6W cells
动物实验 Four- to 6-week old female balb/c athymic (nu+/nu+) mice were purchased from Charles River Laboratories. Mice were acclimatized for 1 week before being injected with cancer cells and injected subcutaneously with 107 H1299 and CALU-3 GEF-R cells that had been resuspended in 200 μL of Matrigel. When established tumors of approximately 75 mm3 in diameter were detected, mice were left untreated or treated with oral administrations of metformin (200 mg/mL metformin diluted in drinking water and present throughout the experiment), gefitinib (150 mg/kg daily orally by gavage), or both for the indicated time periods. Each treatment group consisted of 10 mice. Tumor volume was measured using the formula π/6 × larger diameter × (smaller diameter)2. Tumor tissues were collected from the xenografts and analyzed by Western blotting for the expression and activation of EGFR, AMPK, mitogen-activated protein kinase (MAPK), and S6 [2].
别名 吉非替尼 , ZD1839
纯度 100.00%
分子量 446.91
分子式 C22H24ClFN4O3
CAS No. 184475-35-2

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: 44.7 mg/mL (100 mM)

Ethanol: 4.5 mg/mL (10 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

溶液 1

0.5% methylcellulose+0.2% Tween 80: 12 mg/mL

文献引用

参考文献
1. 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. 2. Morgillo F, et al. Synergistic effects of metformin treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3508-19. 3. K J Williams, et al. ZD1839 (‘Iressa’), a specific oral epidermal growth factor receptor-tyrosine kinase inhibitor, potentiates radiotherapy in a human colorectal cancer xenograft model. Br J Cancer. 2002 Apr 8; 86(7): 1157–1161. 4. Tan J, et al. Tyrosine kinase inhibitors show different anti-brain metastases efficacy in NSCLC: A direct comparative analysis of icotinib, gefitinib, and erlotinib in a nude mouse model. Oncotarget. 2017 Oct 19;8(58):98771-98781. 6. Dhar D, et al. Liver Cancer Initiation Requires p53 Inhibition by CD44-Enhanced Growth Factor Signaling. Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6. 7. Shang J, Ning S, Chen Y, et al. MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer. Acta Pharmacologica Sinica. 2021, 42(1): 120-131 8. Teng J F, Qin D L, Mei Q, et al. Polyphyllin VI, a saponin from Trillium tschonoskii Maxim. induces apoptotic and autophagic cell death via the ROS triggered mTOR signaling pathway in non-small cell lung cancer[J]. Pharmacological Research. 2019: 104396. 9. . circSETD3 Contributes to Acquired Resistance to Gefitinib in Non-Small-Cell Lung Cancer by Targeting the miR-520h/ABCG2 Pathway. Molecular Therapy-Nucleic Acids. 2020 10. Quan C, Chen Y, Wang X, et al. Loss of histone lysine methyltransferase EZH2 confers resistance to tyrosine kinase inhibitors in non-small cell lung cancer. cancer letters. 2020

相关化合物库

该产品包含在如下化合物库中:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-Cancer Compound Library Clinical Compound Library Apoptosis Compound Library Autophagy Compound Library Neuronal Signaling Compound Library Hematopoietic Toxicity Compound Library Tyrosine Kinase Inhibitor Library FDA-Approved Drug Library Immunology/Inflammation Compound Library Cytokine Inhibitor Library Kinase Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Fluorochemical Library Angiogenesis related Compound Library JAK-STAT Compound Library CNS-Penetrant Compound Library Anti-Aging Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library PPI Inhibitor Library Anti-Inflammatory Traditional Chinese Medicine Compound Library Anti-COVID-19 Compound Library Anti-Lung Cancer Compound Library Drug-induced Liver Injury (DILI) Compound Library NMPA-Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Traditional Chinese Medicine Monomer Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Fibrosis Compound Library

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