规格

价格

库存

数量

1 mg

¥ 655

现货

5 mg

¥ 1,650

现货

10 mg

¥ 2,590

现货

25 mg

¥ 3,890

现货

50 mg

¥ 5,580

现货

100 mg

¥ 7,570

现货

200 mg

¥ 9,870

现货

1 mL x 10 mM (in DMSO)

¥ 1,830

现货

生物活性

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) 在约30%的高级浆液性卵巢癌中过表达。ARN-3236在10株卵巢癌细胞系中抑制其生长，IC50范围为0.8至2.6 μmol/L，且ARN-3236的IC50与内源性SIK2表达呈负相关（Pearson r = -0.642, P = 0.03）。ARN-3236还增强了8/10细胞系以及SKOv3ip（P = 0.028）和OVCAR8异种移植瘤对紫杉醇的敏感性。至少在三个细胞系中观察到了协同作用。ARN-3236在间期中断核与中心体的连接，在有丝分裂中阻止中心体分离，导致前期停滞，引发凋亡性细胞死亡和四倍体形成。ARN-3236还抑制了AKT磷酸化并减弱了生存蛋白表达。
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.

化学信息

分子量	336.41
分子式	C₁₉H₁₆N₂O₂S
CAS No.	1613710-01-2
Smiles	COc1ccc(-c2c[nH]c3nccc(-c4ccsc4)c23)c(OC)c1
密度	1.278 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 130 mg/mL (386.43 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.89 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO