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| 品牌 | absin | CAS | 656247-18-6 |
|---|---|---|---|
| 分子式 | C31H33N5O4.C2H6O3S | 纯度 | ≥98% |
| 分子量 | 649.76 | 货号 | abs812859 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | 是一种有效的 VEGFR1/2/3,FGFR1/2/3 和 PDGFRα/β 三 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
BIBF 1120 esylate 656247-18-6
| 产品描述 | |
| 描述 | BIBF 1120 esylate是一种有效的 VEGFR1/2/3，FGFR1/2/3 和 PDGFRα/β 三重抑制剂，IC50 值分别为 34 nM/13 nM/13 nM，69 nM/37 nM/108 nM 和 59 nM/65 nM。 |
| 纯度 | ≥98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | Nintedanib esylate |
| 可溶性/溶解性 | DMSO: 92.85 mg/mL |
| 生物活性 | |
| 靶点 | FGFR |
| In vitro(体外研究) | BIBF 1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC). |
| In vivo(体内研究) | BIBF1120 (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. BIBF1120 is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated. |
| 参考文献 | |
| 参考文献 | [1]. Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 2008, 68(12), 4774-4782. [2]. Roth GJ, 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). J Med Chem, 2009, 52(14), 4466-4480. [3]. Suzuki N, et al. Effect of a novel oral chemotherapeutic agent containing a combination of trifluridine, tipiracil and the novel triple angiokinase inhibitor nintedanib, on human colorectal cancer xenografts. Oncol Rep. 2016 Dec;36(6):3123-3130. |
| 研究领域 | |
| 研究领域 | CancerCancer MetabolismResponse to hypoxia CancerOncoproteins/suppressorsOncoproteinsGrowth factor receptors CardiovascularAngiogenesisEndothelial Cell Markers CardiovascularCardiovascular MarkersCell MarkersEndothelial Cells MetabolismTypes of diseaseCancer MetabolismPathways and ProcessesMetabolism processesHypoxia MicrobiologyInterspecies InteractionHost Virus Interaction NeuroscienceDevelopment NeuroscienceProcesses Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases Stem CellsEndothelial ProgenitorsEndothelial Markers Stem CellsHematopoietic ProgenitorsSurface Molecules Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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