Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
2 mg | 在庫あり | ¥ 8,000 | |||
5 mg | 在庫あり | ¥ 13,000 | |||
10 mg | 在庫あり | ¥ 22,500 | |||
50 mg | 在庫あり | お問い合わせ | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 16,500 |
説明 | 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. |
ターゲット&IC50 | 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 |
In vitro | 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]. |
In vivo | 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]. |
別名 | ON-01910 |
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), Sonification is recommended.
You can also refer to dose conversion for different animals. 詳細
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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 inhibitor