Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rigosertib (ON-01910) 是一种多激酶抑制剂和选择性抗癌剂,通过抑制 PI3K/Akt 途径诱导细胞凋亡,促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。它是一种选择性的非 ATP 竞争性PLK1抑制剂,IC50值为 9 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 297 | 现货 | ||
2 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 997 | 现货 | ||
25 mg | ¥ 1,970 | 现货 | ||
50 mg | ¥ 3,660 | 现货 | ||
100 mg | ¥ 6,230 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 689 | 现货 |
产品描述 | Rigosertib (ON-01910) is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition of the PI3 kinase/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in the cell cycle. |
靶点活性 | CDK1:260 nM, Fyn:182 nM, PDGFR:18 nM, FLK1:42 nM, PLK1:9 nM, PLK2:260 nM, BCR-ABL:32 nM, Src:155 nM |
体外活性 | Rigosertib is a non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib displays cell killing activity against 94 different tumor cell lines (IC50: 50-250 nM), including BT27, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, SW480, and KB cells. Rigosertib also shows inhibition of PLK2, PDGFR, Flt1, BCR-ABL, Fyn, Src, and CDK1 (IC50: 18-260 nM). While in normal cells, such as HFL, PrEC, HMEC, and HUVEC, Rigosertib has little or no effect unless its concentration is greater than 5-10 μM. Rigosertib also inhibits several multidrug-resistant tumor cell lines, including MES-SA, MES-SA/DX5a, CEM, and CEM/C2a (IC50: 50-100 nM). Rigosertib (100-250 nM) causes spindle abnormalities and apoptosis in HeLa cells. Rigosertib (0.25-5 μM) blocks cell cycle progression in G2/M phase in DU145 cells, causes an accumulation of cells containing subG1 content of DNA and activates apoptotic pathways. Rigosertib (50 nM-0.5 μM) induces loss of viability and caspase 3/7 activation in A549 cells. Rigosertib sodium (2 μM) induces apoptosis in chronic lymphocytic leukemia (CLL) cells without toxicity against T-cells or normal B-cells. Rigosertib sodium (2 μM) also abrogates the pro-survival effect of follicular dendritic cells on CLL cells and reduces the SDF-1-induced migration of leukemic cells[3][4][5]. |
体内活性 | Rigosertib (200 mg/kg, i.p.) displays inhibition on tumor growth in a mouse xenograft model of BT20 cells. Rigosertib (250 mg/kg, i.p.) markedly suppresses tumor growth in mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells [3][4]. |
别名 | ON-01910, 瑞格色替 |
分子量 | 451.49 |
分子式 | C21H25NO8S |
CAS No. | 592542-59-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 75 mg/mL (166.12 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2149 mL | 11.0744 mL | 22.1489 mL | 55.3722 mL |
5 mM | 0.443 mL | 2.2149 mL | 4.4298 mL | 11.0744 mL | |
10 mM | 0.2215 mL | 1.1074 mL | 2.2149 mL | 5.5372 mL | |
20 mM | 0.1107 mL | 0.5537 mL | 1.1074 mL | 2.7686 mL | |
50 mM | 0.0443 mL | 0.2215 mL | 0.443 mL | 1.1074 mL | |
100 mM | 0.0221 mL | 0.1107 mL | 0.2215 mL | 0.5537 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。
Rigosertib 592542-59-1 Angiogenesis Apoptosis Cell Cycle/Checkpoint Cytoskeletal Signaling PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors PLK FLT Src PDGFR CDK Bcr-Abl PI3K ON01910 Polo-like Kinase (PLK) Phosphoinositide 3-kinase ON 01910 ON-01910 Inhibitor inhibit 瑞格色替 inhibitor