Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ARN-3236 是一种口服有活性的、具有选择性的盐诱导激酶2 (SIK2)抑制剂,它能够抑制SIK1 (IC50:21.63 nM)、SIK2(IC50<1 nM)和 SIK3(IC50:6.63 nM)。它具有抗肿瘤作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 655 | 现货 | ||
2 mg | ¥ 957 | 现货 | ||
5 mg | ¥ 1,990 | 现货 | ||
10 mg | ¥ 3,130 | 现货 | ||
25 mg | ¥ 4,720 | 现货 | ||
50 mg | ¥ 6,590 | 现货 | ||
100 mg | ¥ 8,880 | 现货 | ||
200 mg | ¥ 11,800 | 现货 | ||
500 mg | ¥ 17,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,830 | 现货 |
产品描述 | ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), (SIK2, SIK1 and SIK3 with IC50s of <1 nM, 21.63 nM and 6.63 nM respectively). ARN-3236 Has anti-cancer activity. |
靶点活性 | SIK1:21.63 nM , SIK2:<1 nM , SIK3:6.63.nM |
体外活性 | Salt-inducible kinase 2 (SIK2) is overexpressed in approximately 30% of high-grade serous ovarian cancers.?ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L, where the IC50 of ARN-3236 was inversely correlated with endogenous SIK2 expression (Pearson r = -0.642, P = 0.03).?ARN-3236 enhanced sensitivity to paclitaxel in 8 of 10 cell lines, as well as in SKOv3ip (P = 0.028) and OVCAR8 xenografts.?In at least three cell lines, a synergistic interaction was observed.?ARN-3236 uncoupled the centrosome from the nucleus in interphase, blocked centrosome separation in mitosis, caused prometaphase arrest, and induced apoptotic cell death and tetraploidy.?ARN-3236 also inhibited AKT phosphorylation and attenuated survivin expression. |
细胞实验 | SIK2 expression was determined in ovarian cancer tissue samples and cell lines.?ARN-3236 was tested for its efficiency to inhibit growth and enhance paclitaxel sensitivity in cultures and xenografts of ovarian cancer cell lines.?SIK2 siRNA and ARN-3236 were compared for their ability to produce nuclear-centrosome dissociation, inhibit centrosome splitting, block mitotic progression, induce tetraploidy, trigger apoptotic cell death and reduce AKT/survivin signaling. |
分子量 | 336.41 |
分子式 | C19H16N2O2S |
CAS No. | 1613710-01-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 130 mg/mL (386.43 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9726 mL | 14.8628 mL | 29.7256 mL | 74.3141 mL |
5 mM | 0.5945 mL | 2.9726 mL | 5.9451 mL | 14.8628 mL | |
10 mM | 0.2973 mL | 1.4863 mL | 2.9726 mL | 7.4314 mL | |
20 mM | 0.1486 mL | 0.7431 mL | 1.4863 mL | 3.7157 mL | |
50 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4863 mL | |
100 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7431 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
ARN-3236 1613710-01-2 Chromatin/Epigenetic PI3K/Akt/mTOR signaling AMPK SIK inhibit ARN 3236 Salt-inducible Kinase (SIK) ARN3236 Inhibitor inhibitor