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- CAS号：
692737-80-7
- 规格：
1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥392.0 |
|---|---|---|---|
| 规格： | 2mg | 产品价格： | ￥242.0 |
| 规格： | 5mg | 产品价格： | ￥364.0 |
| 规格： | 10mg | 产品价格： | ￥582.0 |
| 规格： | 25mg | 产品价格： | ￥1032.0 |
| 规格： | 50mg | 产品价格： | ￥1744.0 |
| 规格： | 100mg | 产品价格： | ￥2896.0 |
| 规格： | 200mg | 产品价格： | ￥4184.0 |
| 规格： | 500mg | 产品价格： | ￥6504.0 |
Product Introduction
Bioactivity
| 名称 | Dovitinib lactate |
| 描述 | Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM). |
| 细胞实验 | Determination of cell proliferation by 3,[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT) assay.?Different leukemic cells were seeded into a 96-well plate at a density of 5×10^3 cells per well and exposed to different concentrations of TKI258, with or without RAD001, in culture medium.?After incubation for indicated time points.Cell-cycle analysis:For cell-cycle analysis, cells were exposed to different concentrations of TKI258, with or without RAD001, in growth medium.?After different culture durations, cells were harvested and fixed in 70% ethanol at 4°C for over 30 min. After incubation for indicated time points, DNA contents were stained.Apoptosis analysis:Cell apoptosis was detected by determining phosphatidylserine expression on the cell surface[1]. |
| 动物实验 | 21-0208 and SK-HEP1 cells as well as patient-derived HCC models were employed to study the antitumor effect of dovitinib.?Changes of biomarkers relevant to FGFR/VEGFR/PDGFR pathways were determined by Western blotting.?Microvessel density, apoptosis and cell proliferation were analyzed by immunohistochemistry[1]. |
| 体外活性 | 所有细胞对TKI258处理极其敏感，体外半数抑制浓度（IC50）值处于nM范围。与mTOR抑制剂RAD001联合使用时，在这些细胞中观察到细胞死亡和细胞增殖的协同效应[1]。SK-HEP1细胞经dovitinib处理后，观察到G2/M细胞周期阻滞、软琼脂中集落形成的抑制以及bFGF诱导的细胞迁移阻断。Dovitinib抑制了FGFR-1、FRS2-α和ERK1/2的基础表达和FGF诱导的磷酸化[2]。 |
| 体内活性 | 在体内，dovitinib 强效抑制了六种HCC细胞系的肿瘤生长。与此同时，抑制血管生成与FGFR/PDGFR-β/VEGFR-2信号通路的失活密切相关。dovitinib 还导致视网膜母细胞瘤蛋白去磷酸化，p-histone H2A-X 和 p27 的上调，以及 p-cdk-2 和 cyclin B1 的下调，进而导致细胞增殖减少和肿瘤细胞凋亡的诱导。在一种正位模型中，dovitinib 强效抑制了原发性肿瘤生长和肺转移，并显著延长了小鼠的存活期[2]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : 2.5 mg/mL (5.18 mM), Solution. DMSO : 25 mg/mL (51.81 mM), Sonication is recommended. |
| 关键字 | VEGFR | Vascular endothelial growth factor receptor | TKI-258 Lactate | TKI258 Lactate | TKI-258 | TKI258 | TKI 258 Lactate | TKI 258 | SCFR | Platelet-derived growth factor receptor | PDGFR | Inhibitor | inhibit | Fms like tyrosine kinase 3 | FLT3 | Fibroblast growth factor receptor | FGFR3 | FGFR | Dovitinib lactate | Dovitinib | Cluster of differentiation antigen 135 | c-Kit | cKit | CHIR-258 Lactate | CHIR258 Lactate | CHIR-258 | CHIR258 | CHIR 258 Lactate | CHIR 258 | CD135 | CD117 |
| 相关产品 | Amlexanox | Gilteritinib | Ribociclib | Lenvatinib | Chloramphenicol | Formononetin | Ferulic Acid | Pazopanib | Dasatinib | Sorafenib | Pexidartinib | Nintedanib esylate |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Colorectal Cancer Compound Library | Kinase Inhibitor Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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7h以上，药物释放按一级反应动力学方式进行。通过控制微囊粒子大小及改变聚乳酸分子量和药物 载体 ，可控制CPFX的释放，以达到延长药物作用的目的。 3 注射剂 CPFX静注剂型有乳酸盐和盐酸盐，国内多家研究单位〔3，4〕研制成功，与进口CPFX作人体药物动力学性质比较，两者主要药动学参数无显著性差异〔5〕。静注CPFX的血清半衰期为5h，若肾功能正常，每12h给药一次不会引起蓄积。与同等剂量口服比较，CPFX静注的Cmax值比口服高，尿中回收率也比口服
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