相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
Icotinib Hydrochloride
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
1204313-51-8
- 规格:
50mg/25mg/10mg/5mg/1mg
| 规格: | 50mg | 产品价格: | ¥5990.0 |
|---|---|---|---|
| 规格: | 25mg | 产品价格: | ¥4278.0 |
| 规格: | 10mg | 产品价格: | ¥2390.0 |
| 规格: | 5mg | 产品价格: | ¥1590.0 |
| 规格: | 1mg | 产品价格: | ¥668.0 |
| 基本信息 | |
| CAS | No.1204313-51-8 |
| 中文名称 | 埃克替尼盐酸盐 |
| 英文名称 | Icotinib Hydrochloride |
| 别名 | ;UNII-JTD32I0J83;CS-0918;BPI-2009H;IcotinibHCl; |
| 分子式 | C22H22ClN3O4 |
| 分子量 | 427.88 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| SMILES | C#CC1=CC(=CC=C1)NC2=NC=NC3=CC4=C(C=C32)OCCOCCOCCO4.Cl |
| 靶点 | EGFR |
| 通路 | Angiogenesis;Protein Tyrosine Kinase/RTK; JAK/STAT Signaling |
| 背景说明 | 是一种新型的、有效的、特异性的 EGFR 抑制剂。 |
| 生物活性 | Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.[1] |
| In Vitro | Incubation with Iconitib at 0.5 μM results in kinase activity inhibition of 91%, 99%, 96%, 61% and 61%, respectively. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. When profiled with 88 kinases, Icotinib only shows meaningful inhibitory activity to EGFR and its mutants. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation (IC50=45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation[1]. |
| 细胞实验 | Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. Icotinib inhibits tumor growth at a rate of 25.2%, 45.6% and 51.5% in the A431 cell line groups; 3.4%, 25.9% and 31.0% in the A549 cell line groups; 49.4%, 52.6% and 67.4% in the H460 cell line groups, and 30.3%, 36.4% and 46.5% in the HCT8 cell line groups, at 30, 60 and 120 mg/kg/dose, respectively[1]. |
| 细胞实验 | Cells (1000/well) are seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37°C. After 24 h, cells are treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 μM for 96 h. Cell proliferation is calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4[1]. |
| 动物实验 | Mice: The effect of three doses of Icotinib (30, 60, and 120 mg/kg/dose p.o. qd) on antitumor activity and survival is determined in mice bearing A431, A549, H460 and HCT8 tumor xenografts. Taxol (30 mg/kg/dose i.p. once a week) is employed in these experiments as a positive control group[1]. |
| 激酶实验 | In the in vitro kinase assays, 2.4 ng/μL EGFR protein is mixed with 32 ng/μL Crk in 25 μL kinase reaction buffer containing 1 μM cold ATP and 1 μCi32P-γ-ATP. The mix is incubated with Icotinib at 0, 0.5, 2.5, 12.5 or 62.5 nM on ice for 10 min followed by incubation at 30°C for 20 min. After quenching with SDS sample buffer at 100°C for 4 min, the protein mix is resolved by electrophoresis in a 10% SDS-PAGE gel. The dried gel is then exposed to detect radioactivity. Quantification is performed by software[1]. |
| 数据来源文献 | [1]. Tan F, et al. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82. |
| 单位 | 瓶 |
风险提示:丁香通仅作为第三方平台,为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全,合理判断,谨慎选购商品,商家和用户对交易行为负责。对于医疗器械类产品,请先查证核实企业经营资质和医疗器械产品注册证情况。
文献和实验三句话读懂一篇 CNS,胎盘其实更像肿瘤组织,可能是遗传缺陷和不良妊娠之源...
春暖花开好时节,周末阳光明媚,坐在樱花树下了解最新学术进展,不失为一种粉色的浪漫! 本周学术君继续为大家带来 CNS 文章,助力科研顺利! 1. Science Translational Medicine:小细胞外囊泡促进血管生成 血管生成在胚胎发育和体内平衡中起着至关重要的作用,干细胞衍生的小细胞外囊泡(sEVs)被证明能促进心肌梗死(MI)后的血管生成。 2021 年 3 月 10 日,浙江大学医学院附属第二医院胡新央、王建安团队与阿拉巴马大学伯明翰分校张建一团队合作在 Science
三句话读懂一篇 CNS:新冠病毒或导致男性过度免疫反应;间歇性禁食能够延寿并降低多种疾病风险
。 该研究通过一项单臂性 II 期探索试验,评估了多种疗法联合应用于 cT4a/bN+ 胃癌新辅助/转化治疗的疗效,基于 ICI 和抗血管生成的新辅助/转化治疗在 cT4a/bN+ 胃癌,尤其是 MSI-H 和 PD-L1 阳性患者中具有良好的疗效和可行性,揭示了几种病理反应的假定生物标志物。 图 5:来源 Nature Communications 6. Nature Aging:用阳光逆转衰老、延长寿命 长生不老是人们的美好夙愿,也是科学家们最想解决的问题。 2022 年 12 月 30
)、神经细胞、细胞外基质(ECM)以及复杂信号分子(细胞因子、趋化因子、生长因子、代谢物)共同构成的动态微环境中。TME 如何从抑制肿瘤转变为促进肿瘤生长、侵袭、血管生成、免疫逃逸和转移的「帮凶」?不同细胞组分间如何通过直接接触或分泌因子进行复杂通讯(crosstalk),形成支持肿瘤的生态位?免疫细胞在 TME 中为何功能失调或耗竭?如何打破 TME 的免疫抑制屏障?TME 的空间结构(如三级淋巴结构的存在与位置)如何影响抗肿瘤免疫应答和预后? 免疫逃逸机制的多样性:肿瘤如何巧妙地躲避或抑制宿主
技术资料暂无技术资料 索取技术资料










