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Chemical Structure| 1225497-78-8 Chemical Structure| 1225497-78-8

Structure of (E/Z)-Rigosertib sodium
CAS No.: 1225497-78-8

Chemical Structure| 1225497-78-8

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Rigosertib Sodium (Random Configuration) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3.

Synonyms: (E/Z)-ON-01910 sodium; ON-01910 (sodium salt); ON-01910

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Product Details of (E/Z)-Rigosertib sodium

CAS No. :1225497-78-8
Formula : C21H24NNaO8S
M.W : 473.47
SMILES Code : O=C([O-])CNC1=CC(CS(=O)(/C=C/C2=C(OC)C=C(OC)C=C2OC)=O)=CC=C1OC.[Na+]
Synonyms :
(E/Z)-ON-01910 sodium; ON-01910 (sodium salt); ON-01910
MDL No. :MFCD11655911
InChI Key :VLQLUZFVFXYXQE-USRGLUTNSA-M
Pubchem ID :23696523

Safety of (E/Z)-Rigosertib sodium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • PLK2

    PLK2, IC50:260 nM

  • PLK1

    PLK1, IC50:9 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa and C33A cells >0.5 μM 24 h Rigosertib induces G2/M arrest and enhances susceptibility to radiation therapy. PMC4005001
DLD1 and HCT116 cells 1 μM 24 h To determine the cytotoxic effects and apoptosis induction. RGS significantly induced apoptosis in both DLD1 and HCT116 cells. PMC8832955
HCC1806 cells 150 nM Induced phosphorylation of histone H3 and G2/M cell cycle arrest PMC11383364
HCC1806 cells 200 nM Induced cell death PMC11383364
Huh7 cells 0.1 to 0.5 μM inhibition of HCV replication PMC9907111
RD cells 2 μM 48 hours Induced apoptosis PMC7867632
SMS-CTR cells 2 μM 48 hours Induced apoptosis PMC7867632
SKNAS cells 2 μM 24 hours Decreased microtubule stability PMC7867632

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Human cervical carcinoma xenografts Intraperitoneal injection 200 mg/kg 3 doses in the first 36 hours and then 2 more doses during radiation therapy Rigosertib, combined with irradiation, showed superior tumor growth delay compared to cisplatin. PMC4005001
Nude mice KRAS-mutant colorectal cancer patient-derived xenograft models Intraperitoneal injection 100 mg/kg 3 weeks To evaluate the inhibitory efficacy on tumor growth. RGS showed a stronger therapeutic effect than the combination standard therapy involving fluoropyrimidine + oxaliplatin/irinotecan + bevacizumab. PMC8832955
Mice subcutaneous xenograft model of HCV replicon-harboring Huh7 cells Intraperitoneal injection 150 mg/kg single dose, observed after 24 hours to validate the anti-HCV activity of rigosertib in vivo PMC9907111
SCID-Beige mice RD xenograft model Intraperitoneal injection 150 mg/kg Twice daily, 5 days per week, until study endpoint Delayed tumor growth and prolonged survival PMC7867632

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.56mL

2.11mL

1.06mL

21.12mL

4.22mL

2.11mL

 

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