货号	规格	价格	上海	北京	武汉	南京
S87051-5mg	99%	￥640.00 S87051-5mg ￥640.00 现货	6 6	-	-	-
S87051-10mg	99%	￥1160.00 S87051-10mg ￥1160.00 现货	4 4	-	-	-
S87051-25mg	99%	￥2720.00 S87051-25mg ￥2720.00 现货	1 1	-	-	-

产品介绍

Filanesib is a selective inhibitor of kinesin spindle protein (KSP, IC50 = 6 nM) with potent anti-proliferative activity.

产品描述：

Filanesib is a selective inhibitor of kinesin spindle protein (KSP, IC50 = 6 nM) with potent anti-proliferative activity.

靶点：

KSP

体内研究：

Filanesib (10, 15, 20, 30 mg/kg, i.p.) is active in UISO-BCA-1 xenograft, and also superior to paclitaxel in mice bearing subcutaneous HT-29, HCT-116, MDA-MB-231 and A2780 xenografts. Filanesib is superior to docetaxel in the androgen receptor-negative prostate cancer xenograft model PC-3. RPMI 8226 tumor xenografts are particularly sensitive to low doses of Filanesib (12.5 mg/kg, i.p.). Filanesib significantly inhibits tumor growth in HL60 and MV4-11 xenografts of SCID mice at concentrations of 27 mg/kg and 20 mg/kg, respectively

细胞实验：

Exponentially growing cells (0.4×10^6/mL) are treated with ARRY-520 for up to 48 hours. For combination, HL-60 and HL-60Bcl-2 cells (0.4×10^6/mL) are incubated with ARRY-520, ABT-737, or both for up to 96 hours. DMSO is used as the control agent. Apoptosis is estimated by flow cytometry measurements of phosphatidylserine with the Annexin-V-FLUOS Staining Kit. Membrane integrity is simultaneously assessed by 7-amino-actinomycin D (7-AAD). To measure changes in the mitochondrial membrane potential (MMP), cells are loaded with CMXRos (300 nM) and MitoTracker Green (500 nM) for 1 hour at 37°C. The loss of MMP is then assessed by measuring CMXRos retention while simultaneously adjusting for mitochondrial mass

动物实验：

Subcutaneous tumor xenografts are allowed to grow to a volume of 250-350 mm3. The mice are randomized into groups of 3-4 based on tumor size and are given a single dose of ARRY-520 i.p. At various time-points after administration of the drug, the mice are euthanized by CO2 inhalation and the tumors excised and placed in 10% neutral buffered formalin. The formalin-fixed tumors are processed and paraffin-embedded by standard procedures. Spindle morphology is analyzed by staining tumor sections for α-tubulin, and apoptosis is analyzed by TUNEL stain. Monopolar/abnormal spindles and TUNEL positive (apoptotic) cells are counted in three ×40 fields from each sample, analyzed using algorithms developed in software

参考文献：

1. Tunquist BJ, et al. Mcl-1 stability determines mitotic cell fate of human multiple myeloma tumor cells treated with the kinesin spindle protein inhibitor ARRY-520. Mol Cancer Ther. 2010 Jul;9(7):2046-56. 2. Woessner R, et al. ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models. Anticancer Res. 2009 Nov;29(11):4373-80. 3. Kim KH, et al. KSP inhibitor ARRY-520 as a substitute for Paclitaxel in Type I ovarian cancer cells. J Transl Med. 2009 Jul 20;7:63. 4. Carter BZ, et al. Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells. Leukemia. 2009 Oct;23(10):1755-62.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.378 ml	11.891 ml	23.782 ml
5 mM	0.476 ml	2.378 ml	4.756 ml
10 mM	0.238 ml	1.189 ml	2.378 ml
50 mM	0.048 ml	0.238 ml	0.476 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)

质量

浓度

体积

分子摩尔量

计算重置

ARRY-520