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Rigosertib

🥰Excellent
Catalog No. T16750Cas No. 592542-59-1
Alias ON-01910

Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase/Akt pathway, promotes histone H2AX phosphorylation, and induces G2/M arrest in the cell cycle.

Rigosertib

Rigosertib

🥰Excellent
Purity: 97.33%
Catalog No. T16750Alias ON-01910Cas No. 592542-59-1
Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase/Akt pathway, promotes histone H2AX phosphorylation, and induces G2/M arrest in the cell cycle.
Pack SizePriceAvailabilityQuantity
2 mg$34In Stock
5 mg$55In Stock
10 mg$97In Stock
50 mgInquiryIn Stock
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Purity:97.33%
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Product Introduction

Bioactivity
Description
Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase/Akt pathway, promotes histone H2AX phosphorylation, and induces G2/M arrest in the cell cycle.
Targets&IC50
CDK1:260 nM, Fyn:182 nM, PDGFR:18 nM, FLK1:42 nM, Src:155 nM, PLK1:9 nM, PLK2:260 nM, BCR-ABL:32 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].
AliasON-01910
Chemical Properties
Molecular Weight451.49
FormulaC21H25NO8S
Cas No.592542-59-1
SmilesC(=C/S(CC1=CC(NCC(O)=O)=C(OC)C=C1)(=O)=O)\C2=C(OC)C=C(OC)C=C2OC
Relative Density.1.332 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 75 mg/mL (166.12 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2149 mL11.0744 mL22.1489 mL110.7444 mL
5 mM0.4430 mL2.2149 mL4.4298 mL22.1489 mL
10 mM0.2215 mL1.1074 mL2.2149 mL11.0744 mL
20 mM0.1107 mL0.5537 mL1.1074 mL5.5372 mL
50 mM0.0443 mL0.2215 mL0.4430 mL2.2149 mL
100 mM0.0221 mL0.1107 mL0.2215 mL1.1074 mL

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