货号	规格	价格	上海	北京	珠海	重庆	武汉
S86234-5mg买3赠1	99.70%	￥365.00 S86234-5mg ￥365.00 现货（买3赠1）	9 9	-	-	-	-
S86234-10mg买3赠1	99.70%	￥595.00 S86234-10mg ￥595.00 现货（买3赠1）	8 8	-	-	-	-
S86234-50mg买3赠1	99.70%	￥1980.00 S86234-50mg ￥1980.00 现货（买3赠1）	7 7	-	-	-	-
S86234-100mg买3赠1	≥99%	￥3300.00 S86234-100mg ￥3300.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively

靶点：

FLT3:1 nM (IC50);c-Kit:2 nM (IC50);FGFR1:8 nM (IC50);FGFR3:9 nM (IC50);VEGFR1:1 nM (IC50);VEGFR3:8 nM (IC50);VEGFR2:13 nM (IC50);PDGFRα:27 nM (IC50);PDGFRβ:210 nM (IC50);VEGFR;FGFR;FLT;PDGFR;c-Kit

体内研究：

Dovitinib (10 mg/kg, 30 mg/kg, 60 mg/kg, p.o.) shows significant antitumor effect in the KMS11-bearing mice model, and the growth inhibition is 48%, 78.5%, and 94% in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment arms, respectively, compared with the placebo-treated mice. Dovitinib demonstrates significant antitumor and antimetastatic activities in HCC xenograft models. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlates with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways. Dovitinib also causes dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which results in a reduction in cellular proliferation and the induction of tumor cell apoptosis

参考文献：

1. Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7), 2941-2948. 2. Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56(3), 595-601.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.072 ml	10.362 ml	20.725 ml
5 mM	0.414 ml	2.072 ml	4.145 ml
10 mM	0.207 ml	1.036 ml	2.072 ml
50 mM	0.041 ml	0.207 ml	0.414 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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Dovitinib Lactate