Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie

Rigosertib [592542-59-1]

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Katalog-Nummer NB-64-07750-10mg

Size : 10mg

Marke : Neo Biotech

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Rigosertib

(Synonyms: ON-01910) Copy Product Info

Synonyms: ON-01910

Catalog No. T16750 Copy Product Info

Purity: 99.53%

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.

Cas No. 592542-59-1

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.53%

Appearance:Solid

Color:White

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	Fyn:182 nM, CDK1:260 nM, PDGFR:18 nM, FLK1:42 nM, BCR-ABL:32 nM, Src:155 nM, PLK1:9 nM, PLK2:260 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].
Synonyms	ON-01910

Chemical Properties

Molecular Weight	451.49
Formula	C₂₁H₂₅NO₈S
Cas No.	592542-59-1
Smiles	C(=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

Storage

Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 75 mg/mL (166.12 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.43 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2149 mL	11.0744 mL	22.1489 mL	110.7444 mL
5 mM	0.4430 mL	2.2149 mL	4.4298 mL	22.1489 mL
10 mM	0.2215 mL	1.1074 mL	2.2149 mL	11.0744 mL
20 mM	0.1107 mL	0.5537 mL	1.1074 mL	5.5372 mL
50 mM	0.0443 mL	0.2215 mL	0.4430 mL	2.2149 mL
100 mM	0.0221 mL	0.1107 mL	0.2215 mL	1.1074 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

SrcRigosertibPolo-like Kinase (PLK)PLK2PLK1PLKPI3KPhosphoinositide 3-kinasePDGFRON01910ON 01910InhibitorinhibitFynFlt1Cdk1BCR-ABLBcrAblApoptosis

Related Tags: Rigosertib chemical structure | Rigosertib in vivo | Rigosertib in vitro | Rigosertib formula | Rigosertib molecular weight