Rigosertib [592542-59-1]
Referentie HY-12037A-10mg
Formaat : 10mg
Merk : MedChemExpress
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
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Rigosertib Chemical Structure
CAS No. : 592542-59-1
This product is a controlled substance and not for sale in your territory.
Based on 5 publication(s) in Google Scholar
Other Forms of Rigosertib:
- Rigosertib sodium In-stock
- (E/Z)-Rigosertib sodium Obtenir un devis
Voir tous les produits spécifiques à Isoform Polo-like Kinase (PLK):
Voir tous les produits spécifiques à Isoform PI3K:
Description |
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle[1][2]. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM[3]. |
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IC50 & Target[1] |
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In Vitro |
Rigosertib is non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM. Rigosertib also exhibits inhibition of PLK2, PDGFR, Flt1, BCR-ABL, Fyn, Src, and CDK1, with IC50 of 18-260 nM. Rigosertib shows cell killing activity against 94 different tumor cell lines with IC50 of 50-250 nM, including BT27, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, SW480, and KB cells. 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. In HeLa cells, Rigosertib (100-250 nM) induces spindle abnormalities and apoptosis[3]. Rigosertib also inhibits several multidrug resistant tumor cell lines, including MES-SA, MES-SA/DX5a, CEM, and CEM/C2a, with IC50 of 50-100 nM. In DU145 cells, Rigosertib (0.25-5 μM) blocks cell cycle progression in G2/M phase, results in an accumulation of cells containing subG1 content of DNA, and activates apoptotic pathways. In A549 cells, Rigosertib (50 nM-0.5 μM) induces loss of viability and caspase 3/7 activation[4]. 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 SDF-1-induced migration of leukemic cells[5]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Rigosertib (250 mg/kg, i.p.) markedly inhibits tumor growth in mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells[3]. Rigosertib (200 mg/kg, i.p.) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells[4]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Essai clinique |
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Masse moléculaire |
451.49 |
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Formule |
C21H25NO8S |
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CAS No. |
592542-59-1 |
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Appearance |
Solid |
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Color |
White to light yellow |
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SMILES |
COC1=CC=C(C=C1NCC(O)=O)CS(/C=C/C2=C(C=C(C=C2OC)OC)OC)(=O)=O.[(E)] |
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Livraison | Room temperature in continental US; may vary elsewhere. |
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Stockage |
-20°C, stored under nitrogen *The compound is unstable in solutions, freshly prepared is recommended. |
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Solvant et solubilité |
In Vitro:
DMSO : 75 mg/mL (166.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
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%
+
%
Tween-80
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%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*The compound is unstable in solutions, freshly prepared is recommended.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Pureté et documentation | |||||||||||||
Références |
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Complete Stock Solution Preparation Table
* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.2149 mL | 11.0744 mL | 22.1489 mL | 55.3722 mL |
5 mM | 0.4430 mL | 2.2149 mL | 4.4298 mL | 11.0744 mL | |
10 mM | 0.2215 mL | 1.1074 mL | 2.2149 mL | 5.5372 mL | |
15 mM | 0.1477 mL | 0.7383 mL | 1.4766 mL | 3.6915 mL | |
20 mM | 0.1107 mL | 0.5537 mL | 1.1074 mL | 2.7686 mL | |
25 mM | 0.0886 mL | 0.4430 mL | 0.8860 mL | 2.2149 mL | |
30 mM | 0.0738 mL | 0.3691 mL | 0.7383 mL | 1.8457 mL | |
40 mM | 0.0554 mL | 0.2769 mL | 0.5537 mL | 1.3843 mL | |
50 mM | 0.0443 mL | 0.2215 mL | 0.4430 mL | 1.1074 mL | |
60 mM | 0.0369 mL | 0.1846 mL | 0.3691 mL | 0.9229 mL | |
80 mM | 0.0277 mL | 0.1384 mL | 0.2769 mL | 0.6922 mL | |
100 mM | 0.0221 mL | 0.1107 mL | 0.2215 mL | 0.5537 mL |