Information ARN-3236 ARN-3236 is a potent, orally available and selective inhibitor of salt-inducible kinase 2 (SIK2) with IC50 of Targets SIK2 (Cell-free assay); SIK3 (Cell-free assay); SIK1 (Cell-free assay) 1 nM; 6.63 nM; 21.63 nM In vitro SIK2 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 vivo The 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
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ARN-3236
Dangerous GoodsCAS number：1613710-01-2 molecular formula：C19H16N2O2S
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | 1H-Pyrrolo[2,3-b]pyridine,3-(2,4-dimethoxyphenyl)-4-(3-thienyl)- | ||
| CAS number | 1613710-01-2 | molecular formula | C19H16N2O2S |
| molecular weight | 336.41 g/mol | Exact mass | - |
| PSA | 75.400 Ų | logp | 3.837 |
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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