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Rigosertib

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Chemical Structure| 592542-59-1 同义名 : ON-01910
CAS号 : 592542-59-1
货号 : A139789
分子式 : C21H25NO8S
纯度 : 98%+
分子量 : 451.49
MDL号 : MFCD09038489
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 80 mg/mL(177.19 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The PI3K/AKT signaling pathway is an essential node in mammalian cells that controls cell growth, migration, proliferation, and metabolism[2]. Rigosertib (RGS) is a PI3K inhibitor that exerts protective effects against tumor progression and cancer-related inflammation. Expression of pro-fibrotic and pro-inflammatory factors including Acta 2, Col 1a1, Col 1a2, IL-1β, TNF-α, INF-γ, and MCP-1 were suppressed in the mice treated with RGS compared to the control group. The protective effects of RGS were mediated by inactivation of PI3K/AKT and NF-kB signaling pathways[3]. Rigosertib significantly inhibited the growth of two RDEB SCC in murine xenograft studies with no apparent toxicity. Mechanistically, rigosertib has been shown to inhibit multiple signaling pathways. Comparison of PLK1 siRNA with MEK inhibition, AKT inhibition, and the microtubule-disrupting agent vinblastine in recessive dystrophic epidermolysis bullosa (RDEB) Squamous cell carcinoma(SCC) shows that only PLK1 reduction exhibits a similar sensitivity profile to rigosertib[4]. Rigosertib induced obvious apoptosis in HEL and K562 cells, and the apoptotic effect was both time-dependent and dose-dependent manner (P<0.05). The low dose of rigosertib inhibited obviously the proliferation of HEL and K562 cells after treatment from 6 to 54h, Rigosertib arrested HEL and K562 cells into G2/M phase. In addition, Rigosertib obviously increased the expression of apoptosis-related proteins such as cleaved caspase 3 and PARP, and reduced the proliferation-related proteins such as BCL-2 and Cyclin D1. Rigosetib inhibited the activation of AKT-GSK signaling through decreasing the expression of AKT, pAKT(Ser473) and GSK-3α/β (S21/9)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.07mL

2.21mL

1.11mL

22.15mL

4.43mL

2.21mL
参考文献

[1]Gumireddy K, et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7(3):275-86.

[2]Saige L Pompura,et al. The PI3K/AKT signaling pathway in regulatory T-cell development, stability, and function. J Leukoc Biol. 2018 Jan 22.

[3]Farzad Rahmani,et al. Rigosertib potently protects against colitis-associated intestinal fibrosis and inflammation by regulating PI3K/AKT and NF-κB signaling pathways. Life Sci. 2020 May 15;249:117470.

[4]Velina S Atanasova,et al. Identification of Rigosertib for the Treatment of Recessive Dystrophic Epidermolysis Bullosa-Associated Squamous Cell Carcinoma. Clin Cancer Res. 2019 Jun 1;25(11):3384-3391.

[5]Feng Xu,et al. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2017 Oct;25(5):1362-1366.