多韦替尼|T6289|TargetMol

Dovitinib
405169-16-6

￥162 1mg 起订

￥413 5mg 起订

￥663 10mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 多韦替尼

英文名称：: Dovitinib

CAS号：: 405169-16-6

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.78%

产品类别：: 抑制剂

货号：: T6289

Product Introduction

Bioactivity

名称	Dovitinib
描述	Dovitinib is an orally active, multi-targeted tyrosine kinase (RTK) inhibitor with anti-tumor effects.
细胞实验	Cell viability is assessed by 3-(4,5-dimethylthiazol)-2,5-diphenyl tetrazolium (MTT) dye absorbance. Cells are seeded in 96-well plates at a density of 5 × 103 (B9 cells) or 2 × 104 (MM cell lines) cells per well. Cells are incubated with 30 ng/mL aFGF and 100 μg/mL heparin or 1% IL-6 where indicated and increasing concentrations of Dovitinib. For each concentration of Dovitinib, 10 μL aliquots of drug or DMSO diluted in culture medium is added. For drug combination studies, cells are incubated with 0.5 μM dexamethasone, 100 nM Dovitinib, or both simultaneously where indicated. To evaluate the effect of Dovitinib on growth of MM cells adherent to BMSCs, 104 KMS11 cells are cultured on BMSC-coated 96-well plates in the presence or absence of Dovitinib. Plates are incubated for 48 to 96 hours. For assessment of macrophage colony-stimulating factor (M-CSF)-mediated growth, 5 × 103 M-NFS-60 cells/well are incubated with serial dilutions of Dovitinib with 10 ng/mL M-CSF and without granulocyte-macrophage colony-stimulating factor (GM-CSF). After 72 hours cell viability is determined using Cell Titer-Glo Assay. Each experimental condition is performed in triplicate. (Only for Reference)
激酶实验	In vitro kinase assays: The inhibitory concentration of 50% (IC50) values for the inhibition of RTKs by Dovitinib are determined in a time-resolved fluorescence (TRF) or radioactive format, measuring the inhibition by Dovitinib of phosphate transfer to a substrate by the respective enzyme. The kinase domains of FGFR3, FGFR1, PDGFRβ, and VEGFR1-3 are assayed in 50 mM HEPES (N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid), pH 7.0, 2 mM MgCl2, 10 mM MnCl2 1 mM NaF, 1 mM dithiothreitol (DTT), 1 mg/mL bovine serum albumin (BSA), 0.25 μM biotinylated peptide substrate (GGGGQDGKDYIVLPI), and 1 to 30 μM adenosine triphosphate (ATP) depending on the Km for the respective enzyme. ATP concentrations are at or just below Km. For c-KIT and FLT3 reactions the pH is raised to 7.5 with 0.2 to 8 μM ATP in the presence of 0.25 to 1 μM biotinylated peptide substrate (GGLFDDPSYVNVQNL). Reactions are incubated at room temperature for 1 to 4 hours and the phosphorylated peptide captured on streptavidin-coated microtiter plates containing stop reaction buffer (25 mM EDTA [ethylenediaminetetraacetic acid], 50 mM HEPES, pH 7.5). Phosphorylated peptide is measured with the DELFIA TRF system using a Europium-labeled antiphosphotyrosine antibody PT66. The concentration of Dovitinib for IC50 is calculated using nonlinear regression with XL-Fit data analysis software version 4.1 (IDBS). Inhibition of colony-stimulating factor-1 receptor (CSF-1R), PDGFRα, insulin receptor (InsR), and insulin-like growth factor receptor 1 (IGFR1) kinase activity is determined at ATP concentrations close the Km for ATP.
体外活性	方法：Dovitinib (CHIR-258)（12.5,25,50,100,200,300,400nM，48小时）处理FGFR3细胞系（KMS11、KMS18、OPM2、H929）和FGFR3细胞系，MTT检测细胞活力。结果：Dovitinib 抑制了 KMS11 (FGFR3-Y373C)、OPM2 (FGFR3-K650E) 和 KMS18 (FGFR3-G384D) 细胞的增殖，IC50 值分别为 90 nM（KMS11 和 OPM2）和 550 nM。[1]
体内活性	方法：Dovitinib (CHIR-258) （10，30，60 mg/kg，口服，每天一次，21天）治疗肿瘤异种移植的模型小鼠，观察体内肿瘤的生长。结果：3个Dovitinib剂量组均观察到显著的抗肿瘤作用，最小有效剂量为10 mg/kg，其中10 mg/kg、30 mg/kg 和 60 mg/kg 治疗组的生长抑制分别为 48%、78.5% 和 94%。[1]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 7.14 mg/mL (18.2 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	Fibroblast growth factor receptor \| Fms like tyrosine kinase 3 \| Vascular endothelial growth factor receptor \| CSF-1 receptor \| FGFR \| inhibit \| CSF-1R \| CHIR 258 \| CSF1R \| VEGFR \| OPM2 \| KMS18 \| RTK \| FLT3 \| SCFR \| Cluster of differentiation antigen 135 \| CD135 \| colony stimulating factor 1 receptor \| CHIR258 \| TKI 258 \| CD117 \| Inhibitor \| c-Kit \| PDGFR \| KMS11 \| c-Fms \| orally \| Dovitinib \| Platelet-derived growth factor receptor \| TKI-258
相关产品	Imatinib \| Amlexanox \| Gilteritinib \| Ribociclib \| Formononetin \| Axitinib \| Ferulic Acid \| Regorafenib \| Pazopanib \| Nintedanib \| Sorafenib \| Regorafenib monohydrate
相关库	经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 膜蛋白靶向化合物库 \| 药物功能重定位化合物库 \| 酪氨酸激酶分子库 \| 抗癌临床化合物库

多韦替尼|||度维替尼|||TKI258|||CHIR-258|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子