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Dovitinib

产品编号 T6289 CAS 405169-16-6

别名: TKI258, 多韦替尼, CHIR-258, 度维替尼

Dovitinib (CHIR-258) 是一种口服有效的、多靶点的酪氨酸激酶 (RTK) 抑制剂，具有抗肿瘤作用。

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Dovitinib, CAS 405169-16-6

规格	价格/CNY	货期
1 mg	￥ 162	现货
5 mg	￥ 413	现货
10 mg	￥ 663	现货
25 mg	￥ 1,330	现货
50 mg	￥ 2,160	现货
100 mg	￥ 3,490	现货
200 mg	￥ 4,980	现货
500 mg	￥ 7,580	现货
1 mL * 10 mM (in DMSO)	￥ 455	现货

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其他形式的 Dovitinib:

Dovitinib lactate hydrate
现货
Dovitinib lactate
现货

选择批次

纯度: 99.78%

纯度: 99.66%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Dovitinib (CHIR-258) (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit, IC50: 1/2 nM), also effective to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs (IC50: 8-13 nM), less potent to EGFR, InsR, EphA2, c-Met, IGF-1R, Tie2, and HER2.
靶点活性	FGFR1/3 (Class IV):8-13 nM, VEGFR1-4 (Class V):8-13 nM
体外活性	Dovitinib强效地抑制了FGF刺激下的WT和F384L-FGFR3表达的B9细胞增长，IC50为25 nM。此外，Dovitinib也能抑制表达各种活化突变体的FGFR3的B9细胞的增殖。有趣的是，对Dovitinib的敏感性在不同的FGFR3突变之间没有明显差异，每种突变的IC50范围为70到90 nM。仅包含载体的IL-6依赖性B9细胞（B9-MINV细胞）对Dovitinib的抑制活动在高达1 μM的浓度下表现出抵抗。Dovitinib对KMS11（FGFR3-Y373C）、OPM2（FGFR3-K650E）和KMS18（FGFR3-G384D）细胞的细胞增殖抑制作用的IC50分别为90 nM（KMS11和OPM2）和550 nM。Dovitinib抑制FGF介导的ERK1/2磷酸化并在表达FGFR3的原发性MM细胞中诱导细胞毒性。BMSCs对用500 nM Dovitinib处理的细胞在与基质共培养时表现出适度的抵抗能力，其生长抑制率为44.6%，而无BMSCs共培养的细胞生长抑制率为71.6%。Dovitinib抑制了M-CSF驱动的小鼠骨髓细胞系M-NFS-60的增殖，其中位有效浓度（EC50）为220 nM。[1] SK-HEP1细胞经Dovitinib处理后，细胞数量剂量依赖性减少，G2/M期阻滞，G0/G1和S期减少，抑制了无锚依赖性生长并阻断了bFGF诱导的细胞移动性。SK-HEP1细胞中Dovitinib的IC50约为1.7 μM。Dovitinib还显著降低了SK-HEP1和21-0208细胞中FGFR-1、FGFR底物2α（FRS2-α）和ERK1/2的基础磷酸化水平，但对Akt无影响。在21-0208 HCC细胞中，Dovitinib显著抑制了bFGF诱导的FGFR-1、FRS2-α、ERK1/2的磷酸化，但对Akt无影响。[2]
体内活性	Dovitinib induces both cytostatic and cytotoxic responses in vivo resulting in regression of FGFR3-expressing tumors.[1] Dovitinib shows a dose- and exposure-dependent inhibition of target receptor tyrosine kinases (RTKs) expressed in tumor xenografts. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlated with inactivation of FGFR/PDGFRβ/VEGFR2 signaling pathways. In an orthotopic model, Dovitinib potently inhibits primary tumor growth and lung metastasis and significantly prolonged mouse survival. [2] Administration of Dovitinib results in significant tumor growth inhibition and tumor regressions, including large, established tumors (500-1,000 mm3). [3]
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.
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)

别名	TKI258, 多韦替尼, CHIR-258, 度维替尼
分子量	392.43
分子式	C21H21FN6O
CAS No.	405169-16-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 28 mg/mL (71.4 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5482 mL	12.7411 mL	25.4823 mL	63.7056 mL
	5 mM	0.5096 mL	2.5482 mL	5.0965 mL	12.7411 mL
	10 mM	0.2548 mL	1.2741 mL	2.5482 mL	6.3706 mL
	20 mM	0.1274 mL	0.6371 mL	1.2741 mL	3.1853 mL
	50 mM	0.051 mL	0.2548 mL	0.5096 mL	1.2741 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Trudel S, et al. Blood, 2005, 105(7), 2941-2948. 2. Huynh H, et al. J Hepatol. 2012, 56(3), 595-601. 3. Lee SH, et al. Clin Cancer Res. 2005, 11(10), 3633-3641. 4. Azab AK, et al. Clin Cancer Res, 2011, 17(13), 4389-4399. 6. Chon HJ, et al. Traf2- and Nck-interacting kinase (TNIK) is involved in the anti-cancer mechanism of dovitinib in human multiple myeloma IM-9 cells. Amino Acids. 2016 Jul;48(7):1591-9.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Dovitinib 405169-16-6 Angiogenesis Tyrosine Kinase/Adaptors PDGFR c-Kit FGFR VEGFR FLT Fibroblast growth factor receptor Fms like tyrosine kinase 3 Vascular endothelial growth factor receptor CSF-1 receptor inhibit CSF-1R CHIR 258 CSF1R TKI258 多韦替尼 OPM2 CHIR-258 KMS18 RTK FLT3 SCFR Cluster of differentiation antigen 135 CD135 colony stimulating factor 1 receptor CHIR258 TKI 258 度维替尼 CD117 Inhibitor KMS11 c-Fms orally Platelet-derived growth factor receptor TKI-258 inhibitor

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Dovitinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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