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| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G125799-50mg |
50mg |
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| G125799-250mg |
250mg |
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| G125799-1g |
1g |
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| G125799-5g |
5g |
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| G125799-10g |
10g |
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| G125799-25g |
25g |
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| G125799-100g |
100g |
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| 别名 | 吉非替尼 |
|---|---|
| 英文别名 | ZD 1839 | AM20090619 | Gefitinib [USAN:INN:BAN] | SY017890 | CHEBI:49668 | nchembio866-comp14 | 4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline | 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)prop |
| 规格或纯度 | Moligand™, ≥99% |
| 英文名称 | Gefitinib (ZD1839) |
| 生化机理 | 吉非替尼是一种表皮生长因子受体(EGFR)-酪氨酸激酶抑制剂,已被证明能增加 HaCaT 细胞中 c-Jun NH2 端激酶(JNK)和 p38 丝裂原活化蛋白激酶(MAPK)的磷酸化。研究表明,吉非替尼可以通过不依赖于表皮生长因子受体的 JNK 激活途径促进角朊细胞凋亡。研究表明,吉非替尼能诱导多种细胞系凋亡,包括 HaCaT 细胞、KG-1 细胞、P39 细胞和原代 CD34+ 骨髓母细胞。口服活性、强效、选择性表皮生长因子受体(EGFR)酪氨酸激酶抑制剂(IC 50 = 33 nM)。抑制表皮生长因子受体刺激的表皮生长因子受体自身磷酸化,抑制体内肿瘤生长。增强细胞毒性药物的疗效。 |
| 储存温度 | 2-8°C储存 |
| 运输条件 | 冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 表皮生长因子受体 erbB1 抑制剂 |
| 备注 | 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。 |
| 产品介绍 |
Gefitinib (ZD1839)是一种EGFR抑制剂,作用于NR6wtEGFR和NR6W细胞中的Tyr1173,Tyr992,Tyr1173和Tyr992,IC50 分别为37 nM,37nM,26 nM和57 nM。An EGFR-tyrosine kinase inhibitor Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. |
| 纯度 | ≥99% |
| ALogP | 4.1 |
|---|
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| PubChem SID | 504756948 |
|---|---|
| 分子类型 | 小分子 |
| IIUPAC Name | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine |
| INCHI | 1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27) |
| InChi Key | XGALLCVXEZPNRQ-UHFFFAOYSA-N |
| Smiles | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 |
| Isomeric SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 |
| 分子量 | 446.9 |
| Reaxy-Rn | 8949523 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8949523&ln= |
| 溶解性 | Soluble in DMSO (89 mg/ml at 25 °C), methanol (20 mg/ml), ethanol (4 mg/ml at 25 °C), DMF (20 mg/ml), and water (<1 mg/ml at 25 °C). |
|---|---|
| 敏感性 | 对热敏感 |
| 比旋光度 | 1.62 |
| 沸点 | 586.8 °C |
| 熔点 | 194.0 to 198.0 °C |
| 分子量 | 446.900 g/mol |
| XLogP3 | 4.100 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 8 |
| 可旋转键计数Rotatable Bond Count | 8 |
| 精确质量Exact Mass | 446.152 Da |
| 单同位素质量Monoisotopic Mass | 446.152 Da |
| 拓扑极表面积Topological Polar Surface Area | 68.700 Ų |
| 重原子数Heavy Atom Count | 31 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 545.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS05, GHS07, GHS08, GHS09 |
|---|---|
| 信号词 | 危险 |
| 危险声明 |
H302: 吞食有害 H315: 引起皮肤刺激 H318: 造成严重的眼睛损伤 H351: 怀疑引起遗传缺陷 H361: 怀疑破坏生育力或未出生的孩子 H373: 通过长时间或反复暴露对器官造成损害 H400: 对水生生物有剧毒 H411: 对水生生物有毒并具有长期持续影响 |
| 预防措施声明 |
P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P264: 处理后要彻底洗手。 P270: 使用本产品时,请勿进食、饮水或吸烟。 P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P321: 特殊处理(请参阅此标签上的...)。 P330: 漱口 P391: 收集溢出物 P302+P352: 如皮肤沾染:用水充分清洗。 P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P203: 使用前,获取、阅读并遵守所有安全说明。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P301+P317: 如果被吞咽:请寻求医疗帮助。 P305+P354+P338: 如果进入眼睛:立即用水冲洗几分钟。取下隐形眼镜(如果有的话),并且操作简单。继续冲洗。 P318: 如果暴露或担心,请就医。 P317: 寻求紧急医疗救助。 P332+P317: 如果出现皮肤刺激:请寻求医疗帮助。 P319: 如果你感到不适,请寻求医疗帮助。 |
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 | |
| 分析证书 | G125799 |
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| 5. Jiali Wang, Xianhai He, Zhirong Jia, Aiwen Yan, Kang Xiao, Shuo Liu, Mengjun Hou, Yaling Long & Xuansheng Ding. (2023) Shenqi Fuzheng injection restores the sensitivity to gefitinib in non-small cell lung cancer by inhibiting the IL-22/STAT3/AKT pathway. Pharmaceutical Biology, 1 (61): (33-41). [PMID:38100532] [10.1080/13880209.2023.2292266] |
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| 7. Yao Liu, Zhichao He, Heng Liang, Minzhen Han, Jinxingyi Wang, Qian Liu, Yanping Guan. (2023) A high-throughput UHPLC-MS/MS method for the determination of eight anti-tumor drugs in plasma. ANALYTICAL BIOCHEMISTRY, 676 (115230). [PMID:37429484] [10.1016/j.ab.2023.115230] |
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| 9. Zhenzhen Pan, Qiufang Chen, Xiulan Zheng, Kai Wang, Yalei Duan, Kang Xiao, Zhirong Jia, Xuansheng Ding. (2023) JuBei Oral Liquid Induces Mitochondria-Mediated Apoptosis in NSCLC Cells. OncoTargets and Therapy, [PMID:32821122] [10.2147/OTT.S254464] |
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| 13. Jianbo Lin, Rujie Zheng, Liping Huang, Yuanrong Tu, Xu Li, Jianfeng Chen. (2022) Folic acid-mediated MSNs@Ag@Geb multifunctional nanocomposite heterogeneous platform for combined therapy of non-small cell lung cancer. COLLOIDS AND SURFACES B-BIOINTERFACES, 217 (112639). [PMID:35759894] [10.1016/j.colsurfb.2022.112639] |
| 14. Yulin Jiang, Jing Wang, Juehan Wang, Yi Zhuang, Lin Qi, Ganjun Feng, Li Zhang. (2022) Fabrication of novel PNIPAM@GO microspheres loaded with dual drugs featuring on-demand drug release capability. JOURNAL OF APPLIED POLYMER SCIENCE, 139 (27): (e52444). [10.1002/app.52444] |
| 15. Pan Zhenzhen, Wang Kai, Wang Xiniao, Jia Zhirong, Yang Yuqi, Duan Yalei, Huang Lianzhan, Wu Zhuo-Xun, Zhang Jian-ye, Ding Xuansheng. (2022) Cholesterol promotes EGFR-TKIs resistance in NSCLC by inducing EGFR/Src/Erk/SP1 signaling-mediated ERRα re-expression. Molecular Cancer, 21 (1): (1-17). [PMID:35303882] [10.1186/s12943-022-01547-3] |
| 16. Yan Zhang, Pei Ma, Zhiguang Duan, Yannan Liu, Yu Mi, Daidi Fan. (2022) Ginsenoside Rh4 Suppressed Metastasis of Lung Adenocarcinoma via Inhibiting JAK2/STAT3 Signaling. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 23 (4): (2018). [PMID:35216134] [10.3390/ijms23042018] |
| 17. Yuqin Zhou, Weitong Hu, Xiangli Zhang, Yi Wang, Wenya Zhuang, Fengzhi Li, Qingyong Li. (2021) Cellular Uptake and Transport Characteristics of FL118 Derivatives in Caco-2 Cell Monolayers. CHEMICAL & PHARMACEUTICAL BULLETIN, 69 (11): (1054-1060). [PMID:34719586] [10.1248/cpb.c21-00467] |
| 18. Fangyin Zhu, Liang Xu, Xudong Li, Ziying Li, Jun Wang, Haijun Chen, Xiumei Li, Yu Gao. (2021) Co-delivery of gefitinib and hematoporphyrin by aptamer-modified fluorinated dendrimer for hypoxia alleviation and enhanced synergistic chemo-photodynamic therapy of NSCLC. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 167 (106004). [PMID:34520834] [10.1016/j.ejps.2021.106004] |
| 19. Zhao-Yang Wang, Hai-Long Wu, Yue-Yue Chang, Tong Wang, Wei Chen, Gao-Yan Tong, Ru-Qin Yu. (2021) Simultaneous determination of nine tyrosine kinase inhibitors in three complex biological matrices by using high-performance liquid chromatography–diode array detection combined with a second-order calibration method. JOURNAL OF SEPARATION SCIENCE, 44 (21): (3914-3923). [PMID:34463059] [10.1002/jssc.202100293] |
| 20. Tianming Dai, Weifan Jiang, Min Wang, Zizheng Guo, Renke Dai. (2021) Influence of two-period cross-over design on the bioequivalence study of gefitinib tablets in beagle dogs. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 165 (105933). [PMID:34260895] [10.1016/j.ejps.2021.105933] |
| 21. Jiang Yuhong, Zhuo Xin, Fu Xiujuan, Wu Yue, Mao Canquan. (2021) Targeting PAR2 Overcomes Gefitinib Resistance in Non-Small-Cell Lung Cancer Cells Through Inhibition of EGFR Transactivation. Frontiers in Pharmacology, 12 (788). [PMID:33967759] [10.3389/fphar.2021.625289] |
| 22. Yue-Yue Chang, Hai-Long Wu, Huan Fang, Tong Wang, Yang-Zi Ouyang, Xiao-Dong Sun, Gao-Yan Tong, Yu-Jie Ding, Ru-Qin Yu. (2021) Comparison of three chemometric methods for processing HPLC-DAD data with time shifts: Simultaneous determination of ten molecular targeted anti-tumor drugs in different biological samples. TALANTA, 224 (121798). [PMID:33379025] [10.1016/j.talanta.2020.121798] |
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| 37. Yilan Huang, Siwei Wang, Xiaojun Zhang, Chen Yang, Sikai Wang, Hongxia Cheng, Aiwu Ke, Chao Gao, Kun Guo. (2024) Identification of Fasudil as a collaborator to promote the anti-tumor effect of lenvatinib in hepatocellular carcinoma by inhibiting GLI2-mediated hedgehog signaling pathway. PHARMACOLOGICAL RESEARCH, 200 (107082). [PMID:38280440] [10.1016/j.phrs.2024.107082] |