ICG1143-0010MG ICG1143-Dovitinib, Lactate Salt

ICG1143-Dovitinib, Lactate Salt

Dovitinib, Lactate Salt，>99%

【英文同义名】：CHIR-258, TKI-258

【中文同义名】：多韦替尼乳酸盐

订购信息：（原装进口，常备现货）

Dovitinib, Lactate Salt是dovitinib的乳酸盐形式，用在dovitinib制剂的生物医学研究中。

Dovitinib一种具有口服活性的小分子，YZIII，IV和V型受体酪氨酸激酶YZ剂，作用于FGFR1(IC₅₀=8 nM)，FGFR3(IC₅₀=9 nM)，VEGFR1(IC₅₀=10 nM)，VEGFR2(IC₅₀=13 nM)，VEGFR3(IC₅₀=8 nM)，PDGFRβ(IC₅₀=27 nM)，FLT3(IC₅₀=1 nM)，c-KIT(IC₅₀=2 nM)和 CSF-1R/c-fms(IC₅₀=36 nM) ^[1]。在SK-HEP1细胞中，dovitinib诱导细胞周期捕获，YZ细胞在集落的形成，同时YZbFGF诱导的细胞迁移。DovitinibYZ肝细胞癌（HCC）移植瘤模型中肿瘤生长，并具有抗迁移活性^[2]。Dovitinib还可以降低肿瘤细胞中磷酸化的PDGFRB和磷酸化的ERK^[3]。Dovitinib与bortezomib，melphalan和dexamethasone等药物联合作用于WM细胞，可以产生累加效应，显著诱导凋亡反应并YZWM细胞增殖^[4]。

靶点

化学特性

Dovitinib, Lactate Salt的具体使用浓度请参考相关文献，并根据自身实验条件（如实验目的，细胞种类，培养特性等）进行摸索和优化。

[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 Apr 1; 105(7):2941-8.

[2] Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012 Mar; 56(3):595-601.

[3] Lee SH, et al. In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models. Clin Cancer Res. 2005 May 15;11(10):3633-41.

[4] Azab AK, et al. FGFR3 is overexpressed waldenstrom macroglobulinemia and its inhibition by Dovitinib induces apoptosis and overcomes stroma-induced proliferation. Clin Cancer Res. 2011 Jul 1;17(13):4389-99.