货号	规格	价格	上海	北京	珠海	重庆	武汉
S83106-1mg	≥99%	￥810.00 S83106-1mg ￥810.00 2-3天	0 货期：2-3天	-	-	-	-
S83106-5mg	≥99%	￥1980.00 S83106-5mg ￥1980.00 2-3天	0 货期：2-3天	-	-	-	-
S83106-10mg	≥99%	￥3100.00 S83106-10mg ￥3100.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .

靶点：

Others

体外研究：

The proliferation rate of PC-3 cells after treatment with ISA-2011B at 10, 20, and 50 μM is significantly reduced to 58.77%, 48.65%, and 21.62% of vehicle-treated controls, respectively. ISA-2011B exhibits the highest binding affinity to PIP5K1α, and to MAP/microtubule affinity-regulating kinase 1 and 4 (MARK1 and MARK4) across 460 kinases. ISA-2011B treatment inhibits PIP5K1α expression by 78.6% in PC-3 cells. ISA-2011B leads to a remarkable reduction in AR-V7 and CDK1 in both nucleus and cytoplasm of 22Rv1 cells. ISA-2011B treatment also abolishes AR expression in the nucleus, without depleting the cytoplasmic AR

体内研究：

ISA-2011B significantly inhibits growth of tumor cells in xenograft mice, and is mediated by targeting PIP5K1α-associated PI3K/AKT and the downstream survival, proliferation, and invasion pathways. Overexpression of AR-V7 increases PIP5K1α, promotes rapid growth of PCa in xenograft mice, whereas inhibition of PIP5K1α by its inhibitor ISA-2011B suppresses the growth and invasiveness of xenograft tumors overexpressing AR-V7. ISA-2011B disrupts protein stabilization of AR-V7 which is dependent on PIP5K1α, leading to suppression of invasive growth of AR-V7-high tumors in xenograft mice

参考文献：

1. Semenas J, et al. The role of PI3K/AKT-related PIP5K1α and the discovery of its selective inhibitor for treatment of advanced prostate cancer. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):E3689-98. 2. Sarwar M, et al. Targeted suppression of AR-V7 using PIP5K1α inhibitor overcomes MDV3100 resistance in prostate cancer cells. Oncotarget. 2016 Sep 27;7(39):63065-63081.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.359 ml	11.797 ml	23.593 ml
5 mM	0.472 ml	2.359 ml	4.719 ml
10 mM	0.236 ml	1.18 ml	2.359 ml
50 mM	0.047 ml	0.236 ml	0.472 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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