ARN-3236
目录号: PL11111 纯度: ≥98%
CAS No. :1613710-01-2
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中文名称
ARN-3236
英文名称
ARN-3236
英文别名
GTPL9581;example 86 [WO2014093383];3-(2,4-dimethoxyphenyl)-4-thiophen-3-yl-1H-pyrrolo[2,3-b]pyridine;ARN-3236
Cas No.
1613710-01-2
分子式
C19H16N2O2S
分子量
336.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ARN-3236 是具有口服活性的盐诱导激酶2 (SIK2) 的选择性抑制剂,其对 SIK2、SIK1 和 SIK3 的 IC50 值分别为 <1 nM、21.63 nM 和 6.63.nM。具有抗肿瘤活性。
生物活性
ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC 50 s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity.
性状
Solid
IC50 & Target[1][2]
SIK2 <1 nM (IC50) SIK1 21.63 nM (IC
体外研究(In Vitro)
ARN-3236 inhibits SIK2 activity with an IC50 <1 nM.
ARN-3236 inhibits cell growth and increases NSC 125973 sensitivity in ovarian cancer cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
ARN-3236 (60 mg/kg, orally) sensitizes ovarian cancer to NSC 125973 in vivo. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SKOv3ip-bearing mice and OVCAR8-bearing mice.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (148.63 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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