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Dovitinib lactate

产品编号 T7104 CAS 692737-80-7

别名: CHIR-258 lactate, 多韦替尼乳酸盐, TKI-258 lactate

Dovitinib lactate (TKI-258 lactate) 是一种多靶点的酪氨酸激酶抑制剂，抑制FLT3，c-Kit，FGFR1/3，VEGFR1/2/3和PDGFRα/β的IC50值分别为 1，2，8/9，10/13/8，27/210 nM。

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Dovitinib lactate, CAS 692737-80-7

规格	价格/CNY	货期
2 mg	￥ 283	现货
5 mg	￥ 455	现货
10 mg	￥ 728	现货
25 mg	￥ 1,290	现货
50 mg	￥ 2,180	现货
100 mg	￥ 3,620	现货
200 mg	￥ 5,230	现货
500 mg	￥ 8,130	现货
1 mL * 10 mM (in DMSO)	￥ 490	现货

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其他形式的 Dovitinib lactate:

Dovitinib lactate hydrate
现货
Dovitinib
现货

选择批次

纯度: 100%

纯度: 99.58%

纯度: 98.44%

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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 lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).
靶点活性	FGFR3:5 nM
体外活性	ALL cells were extremely sensitive to TKI258 treatment with a concentration for 50% inhibition of cell proliferation (IC50) values in the nanomolar range in vitro.?By combination with mTOR inhibitor RAD001, a synergistic effect on cell death and cell proliferation was observed in these cells[1].Treatment of SK-HEP1 cells with dovitinib resulted in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibited basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2[2]
体内活性	In vivo, dovitinib potently inhibited tumor growth of six HCC lines.?Inhibition of angiogenesis correlated with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways.?Dovitinib also caused dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which resulted in a reduction in cellular proliferation and the induction of tumor cell apoptosis.?In an orthotopic model, dovitinib potently inhibited primary tumor growth and lung metastasis and significantly prolonged mouse survival[2].
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].

别名	CHIR-258 lactate, 多韦替尼乳酸盐, TKI-258 lactate
分子量	482.51
分子式	C24H27FN6O4
CAS No.	692737-80-7

存储

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

溶解度

DMSO: 30 mg/mL (62.17 mM)

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	2.0725 mL	10.3625 mL	20.725 mL	51.8124 mL
	5 mM	0.4145 mL	2.0725 mL	4.145 mL	10.3625 mL
	10 mM	0.2072 mL	1.0362 mL	2.0725 mL	5.1812 mL
	20 mM	0.1036 mL	0.5181 mL	1.0362 mL	2.5906 mL
	50 mM	0.0414 mL	0.2072 mL	0.4145 mL	1.0362 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. Eucker J , Zang C , Zhou Y , et al. TKI258, a Multi-tyrosine Kinase Inhibitor Is Efficacious Against Human Infant/Childhood Lymphoblastic Leukemia In Vitro[J]. Anticancer research, 2014, 34(9):4899-4907. 2. Huynh H , Chow P K H , Tai W M , et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma[J]. Journal of Hepatology, 2012, 56(3):0-601.

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 lactate 692737-80-7 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR FLT PDGFR c-Kit CHIR-258 Dovitinib SCFR CHIR-258 Lactate CHIR 258 Lactate CD117 Platelet-derived growth factor receptor TKI258 CHIR-258 lactate TKI 258 CHIR258 CD135 FLT3 CHIR 258 Fms like tyrosine kinase 3 TKI 258 Lactate CHIR258 Lactate TKI258 Lactate 多韦替尼乳酸盐 Inhibitor Cluster of differentiation antigen 135 Vascular endothelial growth factor receptor inhibit TKI-258 TKI-258 lactate TKI-258 Lactate Fibroblast growth factor receptor Dovitinib Lactate inhibitor

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Dovitinib lactate

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

Keywords