货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T96222-1ml	10mM in DMSO	￥486.00 T96222-1ml ￥486.00 现货	3 3	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T96222-1ml

10mM in DMSO

￥486.00

产品描述：

SIK抑制剂;SIK Inhibitors;;InformationARN-3236 ARN-3236 is a potent, orally available and selective inhibitor of salt-inducible kinase 2 (SIK2) with IC50 of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. ARN-3236 induces apoptosis in cancer cells.TargetsSIK2 (Cell-free assay); SIK3 (Cell-free assay); SIK1 (Cell-free assay) 1 nM; 6.63 nM; 21.63 nMIn vitroSIK2 is overexpressed in approximately 30% of high grade serous ovarian cancers. ARN-3236 inhibits growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μM, where the IC50 of ARN-3236 is inversely correlated with endogenous SIK2 expression (Pearson’s r = −0.642, P = 0.03). ARN-3236 enhances sensitivity to paclitaxel in 8 of 10 cell lines. In at least three cell lines a synergistic interaction is observed. ARN-3236 uncouples the centrosome from the nucleus in interphase, blocks centrosome separation in mitosis, causes prometaphase arrest and induces apoptotic cell death and tetraploidy. ARN-3236 also inhibits AKT phosphorylation and attenuates survivin expression.In vivoThe antitumor activity of ARN-3236 is measured using ovarian cancer xenograft model in nu/nu mice. In SKOv3ip xenograft model, ARN-3236 plus paclitaxel produces greater inhibition of tumor growth than any other group and showed statistically significant difference compared to paclitaxel alone (P = 0.028). ARN-3236 also inhibits SIK2 activity and enhances paclitaxel sensitivity in OVCAR8 xenografts.Cell Research(from reference)Cell lines：HEY, A2780, UPN251, OVCAR3, OVCAR5, OVCAR8, ES-2, OC316, SKOv3 and IGROV1 Concentrations：1 μM, 2 μM, 3 μM, 5 μM Incubation Time：16 h, 24 h, 32 h, 48 h

体内研究：

ARN-3236 (60 mg/kg，口服) 在体内增强卵巢癌对 NSC 125973 的敏感性。

参考文献：

1. Lombardi MS, et al. SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J Leukoc Biol. 2016 May;99(5):711-21.
2. Zhou J, et al. A Novel Compound ARN-3236 Inhibits Salt-Inducible Kinase 2 and Sensitizes Ovarian Cancer Cell Lines and Xenografts. Clin Cancer Res. 2017 Apr 15;23(8):1945-1954.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.973 ml	14.863 ml	29.726 ml
5 mM	0.595 ml	2.973 ml	5.945 ml
10 mM	0.297 ml	1.486 ml	2.973 ml
50 mM	0.059 ml	0.297 ml	0.595 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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