Gefitinib (ZD1839)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Gefitinib（ZD1839，Iressa）是一种有效的和可口服的表皮生长因子受体（EGFR）酪氨酸激酶小分子抑制剂，在A431膜制备物和杆状病毒裂解物中的IC50值分别为0.033 μM和0.027 μM。Gefitinib与EGFR激酶的ATP结合位点结合，干扰三磷酸腺苷的结合，从而抑制EGFR酪氨酸激酶活性和EGFR信号转导。Gefitinib在广泛的人类肿瘤类型中具有抗血管生成活性，包括头颈癌、前列腺癌、乳腺癌、卵巢癌、结肠癌、小细胞肺癌和非小细胞肺癌。而且，geftinib也可减少细胞增殖，诱导细胞周期停滞，增加细胞凋亡。
参考文献：
M. Ranson and S. Wardell. Gefitinib, a novel, orally administered agent for the treatment of cancer. Journal of Clinical Pharmacy and Therapeutics (2004) 29, 95-103
Joachim Von Pawel. Gefitinib (Iressa, ZD1839): a novel targeted approach for the treatment of solid tumors. Bull Cancer 2004; 91(5): E70-E76
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- 2. Priscilla Cheung, Jordi Xiol, et al. "Regenerative Reprogramming of the Intestinal Stem Cell State via Hippo Signaling Suppresses Metastatic Colorectal Cancer." Cell Stem Cell. 2020 Oct 1;27(4):590-604.e9. PMID: 32730753
- 3. Lina Zhao, Ting Qiu, et al. "SGCE Promotes Breast Cancer Stem Cells by Stabilizing EGFR." Adv Sci (Weinh). 2020 Jun 8;7(14):1903700. PMID: 32714745
- 4. Lee YC, Wang LJ, et al. "Inhibition of EGFR pathway promotes the cytotoxicity of ABT-263 in human leukemia K562 cells by blocking MCL1 upregulation." Biochem Pharmacol. 2020;178:114047. PMID: 32446890
- 5. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID: 31063758
- 6. She K, Fang S, et al. "SCD1 is required for EGFR-targeting cancer therapy of lung cancer via re-activation of EGFR/PI3K/AKT signals." Cancer Cell Int. 2019 Apr 18;19:103. PMID: 31019378
- 7. Chen Z, Tian D, et al. "Apigenin Combined With Gefitinib Blocks Autophagy Flux and Induces Apoptotic Cell Death Through Inhibition of HIF-1α, c-Myc, p-EGFR, and Glucose Metabolism in EGFR L858R+T790M-Mutated H1975 Cells." Front Pharmacol. 2019 Mar 22;10:260. PMID: 30967777
- 8. Huang SZ, Wei MN, et al. "Targeting TF-AKT/ERK-EGFR Pathway Suppresses the Growth of Hepatocellular Carcinoma." Front Oncol. 2019 Mar 15;9:150. PMID: 30931258
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 446.90 |
| Cas No. | 184475-35-2 |
| Formula | C22H24ClFN4O3 |
| Synonyms | Iressa,ZD-1839,Gefitinib |
| Solubility | ≥22.34 mg/mL in DMSO; insoluble in H2O; ≥2.48 mg/mL in EtOH with ultrasonic |
| Chemical Name | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验: [1] | |
|
细胞系 |
BT-474细胞 |
|
制备方法 |
该化合物在DMSO中的溶解度大于10 mM，若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应条件 |
1 μM，24 hours |
|
实验结果 |
用1 μM ZD1839处理BT-474细胞24小时，G1分数从74增加至88％，S期细胞的比例从15降至4％。G1中细胞积累的同时，用磷酸特异性抗体测量，活性Akt和MAPK完全消失，总Akt和MAPK的含量没有变化。与Akt活性的抑制一致，Akt激酶的靶标GSK-3β的磷酸化减少。细胞周期蛋白D1和Cdk4也减少，而Cdk抑制剂p27的蛋白质水平上调。 |
| 动物实验: [2] | |
|
动物模型 |
注射BT-474细胞的雌性Balb/C无胸腺裸鼠 |
|
给药剂量 |
口服，200 mg/kg/day |
|
实验结果 |
将小鼠随机分配为未治疗、ZD1839、Herceptin或两者组合。ZD1839完全抑制肿瘤生长，但没有诱导完全消退。单独的Herceptin处理，诱导7个小鼠中的2个完全消退，而药物组合使用导致8个小鼠中的3个得到完全缓解。小鼠没有表现出治疗相关毒性。用ZD1839加上Herceptin治疗的三只小鼠的肿瘤完全消退，在停止治疗后保持无肿瘤状态大于6个月，在尸体解剖时没有可检测的肿瘤。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1] Moulder S L, Yakes F M, Muthuswamy S K, et al. Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo. Cancer research, 2001, 61(24): 8887-8895. |
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| Description | Gefitinib (ZD-1839)是EGFR的抑制剂，作用于NR6wtEGFR和NR6W细胞中的EGFR Tyr1173、Tyr992、Tyr1173和Tyr992，IC50值分别为37 nM、37nM、26 nM 和57 nM。 | |||||
| 靶点 | Tyr1173 (NR6wtEGFR cells) | Tyr992 (NR6wtEGFR cells) | Tyr1173 (NR6W cells) | Tyr992 (NR6W cells) | ||
| IC50 | 37 nM | 37nM | 26 nM | 57 nM | ||
质量控制和MSDS
- 批次:
化学结构
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