Nintedanib (BIBF 1120)
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ￥636.00 | 现货 | |
| 5mg | ￥500.00 | 现货 | |
| 10mg | ￥700.00 | 现货 | |
| 25mg | ￥1300.00 | 现货 | |
| 50mg | ￥1950.00 | 现货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
Nintedanib (BIBF 1120)是一种吲哚啉酮衍生的具口服活性的三重激酶抑制剂，对血管内皮生长因子受体（VEGFR1/2/3）、成纤维细胞生长因子受体（FGFR1/2/3 ）和血小板衍生生长因子受体（PDGFRα/β）具有抑制作用，在纳摩尔（IC50, 20-100 nmol/L）范围时通过阻断这些受体介导的信号途径，具有有效的抗血管生成活性[1，2]。
Nintedanib (BIBF 1120)可用于特发性肺纤维化治疗的临床研究，因为这些受体可能参与肺纤维素化的发病机制[3，4]。作为一种新型的血管生成抑制剂，Nintedanib也在各种癌症模型中被广泛评估，其通过抑制肿瘤血管形成，发挥显著的抗肿瘤活性[5-7]。
为进一步评估其在多个肿瘤中的抗肿瘤作用，目前Nintedanib已经进入很多癌症的临床试验中,包括非小细胞肺癌、卵巢癌、结直肠癌、肝癌和许多其他恶性实体瘤。此外，也进行了Nintedanib与其它治疗的联合用药疗法试验，比如在不同肿瘤模型中测试Nintedanib与docetaxel和afatinib联合用药，最常见的药物相关不良反应有腹泻、恶心、呕吐和嗜睡[7]。
参考文献：
[1] Hilberg, F. et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer research 68, 4774-4782, doi:10.1158/0008-5472.CAN-07-6307 (2008).
[2] Roth, G. J. et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). Journal of medicinal chemistry 52, 4466-4480, doi:10.1021/jm900431g (2009).
[3] Wollin, L. , Maillet, I., Quesniaux, V., Holweg, A. & Ryffel, B. Antifibrotic and Anti-inflammatory Activity of the Tyrosine Kinase Inhibitor Nintedanib in Experimental Models of Lung Fibrosis. The Journal of pharmacology and experimental therapeutics 349, 209-220, doi:10.1124/jpet.113.208223 (2014).
[4] Antoniu, S. A. Nintedanib (BIBF 1120) for IPF: a tomorrow therapy Multidisciplinary respiratory medicine 7, 41, doi:10.1186/2049-6958-7-41 (2012).
[5] Santos, E. S., Gomez, J. E. & Raez, L. E. Targeting angiogenesis from multiple pathways simultaneously: BIBF 1120, an investigational novel triple angiokinase inhibitor. Investigational new drugs 30, 1261-1269, doi:10.1007/s10637-011-9644-2 (2012).
[6] Wei, X. W., Zhang, Z. R. & Wei, Y. Q. Anti-angiogenic drugs currently in Phase II clinical trials for gynecological cancer treatment. Expert opinion on investigational drugs 22, 1181-1192, doi:10.1517/13543784.2013.812071 (2013).
[7] Mross, K. et al. Phase I study of the angiogenesis inhibitor BIBF 1120 in patients with advanced solid tumors. Clinical cancer research : an official journal of the American Association for Cancer Research 16, 311-319, doi:10.1158/1078-0432.CCR-09-0694 (2010).
[8] Rolfo, C. et al. BIBF 1120/ nintedanib : a new triple angiokinase inhibitor-directed therapy in patients with non-small cell lung cancer. Expert opinion on investigational drugs 22, 1081-1088, doi:10.1517/13543784.2013.812630 (2013).
[9] Tai, W. T. et al. Nintedanib (BIBF-1120) inhibits hepatocellular carcinoma growth independent of angiokinase activity. Journal of hepatology, doi:10.1016/j.jhep.2014.03.017 (2014).
[10] Reck, M. et al. Docetaxel plus nintedanib versus docetaxel plus placebo in patients with previously treated non-small-cell lung cancer (LUME-Lung 1): a phase 3, double-blind, randomised controlled trial. The lancet oncology 15, 143-155, doi:10.1016/S1470-2045(13)70586-2 (2014).
[11] Bouche, O. et al. Phase II trial of weekly alternating sequential BIBF 1120 and afatinib for advanced colorectal cancer. Anticancer research 31, 2271-2281 (2011).
产品性质
| 物理外观 | A solid |
| CAS号 | 656247-17-5 |
| 分子式 | C31H33N5O4 |
| 分子量 | 539.62 |
| 小分子别名 | Nintedanib |
| 化学名称 | methyl (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate |
| 溶解度 | insoluble in H2O; insoluble in EtOH; ≥5.34 mg/mL in DMSO |
| SMILES | CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)NC(=C3C4=C(C=C(C=C4)C(=O)OC)NC3=O)C5=CC=CC=C5 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | BIBF 1120是一种有效的三重激酶抑制剂，对VEGFR1/2/3、FGFR1/2/3 和 PDGFRα/β的IC50值分别为34 nM/13 nM/13 nM、69 nM/37 nM/108 nM和59 nM/65 nM。 | ||
| 靶点 | VEGFR1/2/3 | FGFR1/2/3 | PDGFRα/β |
| 生物活性数据 | 34 nM/13 nM/13 nM | 69 nM/37 nM/108 nM | 59 nM/65 nM |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 4 篇科研文献
- 1. da Silva RF, Banzato TP, et al. "Antiangiogenic therapy with Nintedanib affects hypoxia, angiogenesis and apoptosis in the ventral prostate of TRAMP animals." Cell Tissue Res. 2019 Aug 31. PMID:31473819
- 2. Mateus PAM, Kido LA, et al. "Association of anti-inflammatory and antiangiogenic therapies negatively influences prostate cancer progression in TRAMP mice." Prostate. 2018 Dec 25. PMID:30585351
- 3. Pangrazi EN, da Silva RF, et al. "Nintedanib treatment delays prostate dorsolateral lobe cancer progression in the TRAMP model: Contribution to the epithelial-stromal interaction balance." Cell Biol Int. 2017 Oct 5. PMID:28980742
- 4. Janelle DeJong."Determination of Anti-Fibrotic Effects of Possible Scar-Collagen Antagonists on TGF-β1 Treated Dermal Fibroblasts." 2017 Feb 1;7(2):203-217. eCollection 2017.
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