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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
见说明书
- 保质期：
＞1年
- 英文名：
Gefitinib Free Base
- 库存：
期货2-3周
- 供应商：
上海经科化学科技有限公司
- CAS号：
184475-35-2
- 规格：
1g
供应商：上海经科化学科技有限公司
服务热线：400-0199-638
QQ:472482400(上海经科）
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本试剂(吉非替尼)
仅供科研实验使用,不得用于其他用途！
货 号：LC1-G-4408
名 称：吉非替尼
别 名：Gefitinib Free Base
C A S ：184475-35-2
分子量：446.9
分子式：C22H24ClFN4O3
纯 度：HPLC/TLC:>99%
说 明：Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO, up to about 100 mg/mL; very poorly soluble in water or ethanol. Disposal: A.
文 献：EGFR tyrosine kinase inhibitor that binds to the ATP-binding site of the enzyme. The functions of the EGFR tyrosine kinase in activating the Ras signal transduction cascade and malignant cell growth are thus inhibited. It has been shown that a mutation in the EGFR tyrosine kinase domain is responsible for activating anti-apoptotic pathways in gefitinib-sensitive non-small cell lung cancers. These mutations tend to increase sensitivity to tyrosine kinase inhibitors including gefitinib and erlotinib. The adenocarcinoma subset of non-small cell lung cancer histologies often have these mutations, which are commonly found in Asians, women, and non-smokers. Pao, W., et al. "EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib." Proc. Natl. Acad. Sci. USA 101: 13306-13311 (2004). Sordella, R., et al. "Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways." Science 305: 1163-1167 (2004). The IC50 values for gefitinib for inhibiting HT-29 and LoVo cell growth were 23.6 - >100 µM and 7.3 - 48.5 µM, respectively, when the exposure times are from 18 hours to 3 days. A time-dependent reduction in IC50 was observed for gefitinib, with the IC50 after 3 days of exposure being 4-8 fold less after 18 hours of exposure. Azzariti, A., et al. "Prolonged exposure of colon cancer cells to the epidermal growth factor receptor inhibitor gefitinib (Iressa™) and to the antiangiogenic agent ZD6474: Cytotoxic and biomolecular effects." World J. Gastroenterol. 12: 5140-5147 (2006). Gefitinib was found to be a potent inhibitor of EGFR kinase (Ki = 0.40 nM), but much weaker against ErbB-2 kinase (Ki = 870 nM) and ErbB-4 kinase (Ki = 1.1 µM). Wood, E.R., et al. "A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib), Relationships among Protein Conformation, Inhibitor Off-Rate, and Receptor Activity in Tumor Cells." Cancer Res. 64: 6652-6659 (2004). The IC50 of gefitinib for cells grown in the absence (IC50 = 8.8 µM) of EGF is >100-fold weaker than that in the presence (IC50 = 0.054 µM) of EGF. Gefitinib selectively inhibited EGF-stimulated growth of HUVECs (IC50 = 0.03 - 0.1 µM) compared with FGF- or VEGF-stimulated growth (IC50 = 1 - 3 µM for both). Enzyme kinetic studies were used to determine the characteristics of gefitinib inhibition of EGFR tyrosine kinase. Gefitinib is a competitive inhibitor with respect to ATP (Ki = 2.1 nM) when the peptide substrate concentration was fixed at 2 mM (6-fold higher than the Km) and the ATP concentration was varied. Gefitinib showed noncompetitive kinetics (Ki = 15.0 nM) when the ATP concentration was 50 µM (6-fold higher than the Km) and the peptide concentration was varied. Wakeling, A.E., et al. "ZD1839 (Iressa), An Orally Active Inhibitor of Epidermal Growth Factor Signaling with Potential for Cancer Therapy." Cancer Res. 62: 5749-5754 (2002).
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文献和实验别小看EGFR的耐药，这可是KEGG上独立的一个信号通路……
，和2）旁路途径的激活。上次说过，EGFR可以通过与HER2或者本身的二聚体，激活下游的JAK/STAT、PI3K/AKT和MAPK信号通路（MAPK信号通路是通过EGFR激活Shc→Grb2后激活的，这个上次漏讲了）：常用的抑制剂类药物，吉非替尼和厄洛替尼可以结合并抑制EGFR的活性：但当EGFR氨基酸790位的苏氨酸突变成了甲硫氨酸的话，吉非替尼和厄洛替尼就无法结合上EGFR，也就无法抑制EGFR的下游通路，产生了耐药性。在旁路途径中，常见的还有原癌基因c-Met的激活，会导致Her3的磷酸化，进一步
肺癌是英国第二常见的癌症类型，每年有3.8万人被诊断出肺癌。针对表皮生长因子(EGF)受体的生物疗法被用于治疗EGF受体突变的肺癌患者。这些EGF受体抑制剂，包括阿法替尼、西妥昔单抗、吉非替尼和埃罗替尼，与化疗相比与改善无进展生存相关。然而，最终肿瘤会产生耐药性，这通常是由于EGF受体的进一步突变造成的。 在《BMC医学》发表的一项新研究中，Jacques De Greve和他的同事们探索了克服耐药性问题的新策略，并表明使用siRNA干扰EGF受体基因会导致肺癌细胞死亡。在orderChen
。 8. 酶制剂及酶抑制剂：如酪氨酸激酶的小分子抑制剂伊马替尼（Gleevec）、吉非替尼（Iressa）、艾罗替尼（Tarceva）；蛋白酶体抑制剂万柯（Velcade）。 9. 某些微生物及其有效成份的制剂：如卡介苗(BCG)、短小棒状杆菌(CP)、链球菌(0K432)、济南假单胞菌等。 10. 植物药包括中药的有效成份：如香菇多糖、云芝多糖、黄芪多糖、刺五加多糖、扶正女贞素LL-E、枸杞多糖、淫羊藿多糖、商陆多糖、人参总皂苷、冬虫夏草等。 11. 有机酸及小分子合成剂：如左旋
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