ARRY-520

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抑制剂描述：

产品名称：ARRY-520

产品别名：见爱必信官网

英文别名：ARRY-520

靶点：Kinesin

CAS：885060-09-3

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

ARRY-520 is a potent and selective kinesin spindle protein (KSP) inhibitor with an IC50 of 15 nM for A2780, CP70 and 01-28 cell lines in vitro. ARRY-520 had low nanomolar antiproliferative activity in tumor cell lines. ARRY-520 effectively reduced cell viability in a time-dependent manner in the Type II EOC cell lines A2780, CP70, and 01–28 but had minimal effect on Paclitaxel-resistant Type I EOC cell lines R182, 01–19b, and R1140. In addition, following ARRY-520 treatment, a significant increase in the activity of caspases- 8, 9, and 3 was observed in a time-dependent manner.ARRY-520 is able to induce the activation of caspase-2 in a time-dependent manner similar to that observed with the other caspases-9, -8, and -3. ARRY-520 is able to down-regulate the constitutive MCP-1 secretion. In addition, ARRY-520 induced a decrease in tumor kinetics in a dose-dependent manner.

溶解性：DMSO ：> 10 mM

体外研究：

ARRY-520 retains activity in multidrug-resistant cell lines. The EC50s of ARRY-520 for inhibition of proliferation of HCT-15, NCI/ADR-RES and K562/ADR cells are 3.7, 14 and 4.2 nM respectively. ARRY-520 (10 nM) blocks a majority of cells in mitosis with the monopolar spindle structure typical of KSP inhibition. ARRY-520 (10 nM) induces mitotic arrest as judged by both increased phosphorylation of histone H3 (pHH3) and accumulation of cyclin B1 in four cells. ARRY-520 and Paclitaxel exhibit the same cytotoxic effect on Type I and II cells. The GI50 at 48 h for Type II EOC cells is 0.0015 μM for ARRY-520. For Type I EOC cells, the GI50 at 48 h is > 3 μM for ARRY-520. ARRY-520 (1 nM) induces significant G2M cell cycle block in OCI-AML3 cells at 24 hours.

体内研究：ARRY-520 (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. ARRY-520 is superior to docetaxel in the androgen receptor-negative prostate cancer xenograft model PC-3, and is also superior to docetaxel in the DU145 prostate xenograft model. RPMI 8226 tumor xenografts are particularly sensitive to low doses of ARRY-520 (12.5 mg/kg, i.p.). ARRY-520 significantly inhibits tumor growth in HL60 and MV4-11 xenografts of SCID mice at concentrations of 27 mg/kg and 20 mg/kg, respectively.

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