现货,Dovitinib (TKI-258)，目录号S1018,CAS号:405169-16-6，FltYZ剂，美国Selleck

信号转导通路:  受体酪氨酸激酶(RTK) >> Flt >> Flt YZ剂 >> Dovitinib (TKI-258)
http://selleck.cn/dovitinib-tki258-S1018.html

技术数据:
分子量(MW): 392.43 
化学式: 
C21H21FN6O
溶解度: DMSO ≥115mg/mL   Water ≥115mg/mL   Ethanol <1mg/mL
纯度: >99%
稳定性: at -20℃
CAS号: 405169-16-6

生物活性
Dovitinib is a highly potent, novel multitargeted growth factor receptor kinase inhibitor with IC50 of 1, 2, 5, 10, 8, 27, 36 nM for FLT3, c-KIT, FGFR, VEGFR1/2/3, PDGFRß and CSF-1R, respectively. [1] Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 values of 25 nM. In addition, Dovitinib inhibits proliferation of B9 cells expressing each of the various activated mutants of FGFR3. IL-6-dependent B9 cells containing vector only (B9-MINV) are used to detect nonspecific toxicity. B9-MINV cells are resistant to the inhibitory activity of Dovitinib at concentrations up to 1 μM. [1] Dovitinib inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively. Dovitinib prevents FGF-mediated ERK1/2 phosphorylation and induces cytotoxicity in FGFR3-expressing primary MM cells. BMSCs does confer a modest degree of resistance with 44.6% growth inhibition for cells treated with 500 nM Dovitinib and cultured on stroma compared with 71.6% growth inhibition for cells grown without BMSCs. Dovitinib inhibits proliferation of M-NFS-60, an M-CSF growth-driven mouse myeloblastic cell line with a median effective concentration (EC50) of 220 nM. [1] Treatment of SK-HEP1 cells with Dovitinib results in a dose-dependent reduction in cell number and G2/M phase arrest with reduction in the G0/G1 and S phases, inhibition of anchorage-independent growth and blockage of bFGF-induced cell motility. The IC50 for Dovitinib in SK-HEP1 cells is approximately 1.7 μM. Dovitinib also significantly decreases the basal phosphorylation levels of FGFR-1, FGFR substrate 2α (FRS2-α) and ERK1/2 but not Akt in both SK-HEP1 and 21-0208 cells. In 21-0208 HCC cells, Dovitinib significantly prevents bFGF-induced phosphorylation of FGFR-1, FRS2-α, ERK1/2 but not Akt. [2] Dovitinib induces both cytostatic and cytotoxic responses in vivo resulting in regression of FGFR3-expressing tumors. [1] Administration of Dovitinib results in significant tumor growth inhibition and tumor regressions, including large, established tumors (500-1,000 mm3). [3] Dovitinib shows a dose- and exposure-dependent inhibition of target RTKs expressed in tumor xenografts. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlated 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. In an orthotopic model, Dovitinib potently inhibits primary tumor growth and lung metastasis and significantly prolonged mouse survival. [2] Dovitinib has entered in a phase II clinical trial for the treatment of adenoid cystic carcinoma.

参考文献
CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Trudel S, et al. Blood 2005;105(7), 2941-2948
Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. Huynh H, et al. J Hepatol 2012;56(3), 595-601
In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models. Lee SH, et al. Clin Cancer Res 2005;11(10), 3633-3641

如果需要长期保存，请于零下二十度低温保存。
禁止用于人体及ZL！

特定的存储和包装每个产品的信息在产品说明书上都有注明 。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20 ° C ，抗体及蛋白等产品建议-60℃。YZ剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。

 

退换货政策        

 1、 退换货只针对已付款用户。一张订单Selleck只提供一次退换货服务，为了确保您的权益，请考虑周全后与我们联系。        
 2、请您确保退换货时，商品、配件、赠品及各种包装完整。        
 3、因您个人原因造成的商品损坏（如自行使用、分装、受潮、变质、非原物品的等）将不予退换。          
 4、Selleck目前只支持商品一换一服务，换货时无法加定商品。        
 5、如您购买商品时Selleck上海办事处已向您提供发票，则办理退货或订单金额发生变更的换货时，请将发票随商品一同返还给Selleck上海办事处赛导通生物科技（南京）有限公司，请您妥善保管发票，如发票丢失，将无法办理退换货。        
 6、您的订单若办理退换货，运费金额会在您的实际退款中扣除。