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533575 Rigosertib - CAS 592542-60-4 - Calbiochem

533575
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Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₁H₂₄NNaO₈S 592542-60-4

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      Description
      OverviewA cell-permeable, nontoxic benzylstyrylsulfone based compound with anti-tumor and radiosensitizing properties. Potently suppresses PI 3-K/Akt/mTOR signaling pathway and activates Cdc25C phosphatases. Acts as an allosteric, substrate-competitive, and reversible inhibitor of multiple protein kinases (IC50 = 32, 42, 182, 18 and 155 nM against Bcr-Abl, Flt1, Fyn, PDGFR, and Src, respectively). Induces DNA damage and blocks microtubule formation. Also shown to cause mitotic arrest and apoptosis in multiple types of cancer cells (GI50 = 30-200 nM) and blocks cell cycle at G2/M phase. Effective against several multi-drug resistance tumor cells (IC50 = 50-100 nM). Suppresses the growth of BT20 tumor xenografts in mice and improves their survival rate (200 mg/kg, i.v. Q2D X 20 schedule). However, it displays limited oral bioavailability.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533575
      Brand Family Calbiochem®
      SynonymsSodium (E)-2-(2-methoxy-5-((2,4,6-trimethoxystyrylsulfonyl)methyl)phenylamino)acetate, ON01910, Na, Estybon
      References
      ReferencesLu, T., et al. 2015. Mol. Pharmacol. 87, 18.
      Ramana Reddy, M.V., et al. 2011. J. Med. Chem. 54, 6254.
      Gumireddy, K., et al. 2005. Cancer Cell 7, 275.
      Product Information
      CAS number592542-60-4
      FormOff-white solid
      Hill FormulaC₂₁H₂₄NNaO₈S
      Chemical formulaC₂₁H₂₄NNaO₈S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPI 3-K/Akt/mTOR signaling
      Primary Target IC<sub>50</sub>32, 42, 182, 18 and 155 nM against Bcr-Abl, Flt1, Fyn, PDGFR, and Src, respectively
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Rigosertib - CAS 592542-60-4 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Lu, T., et al. 2015. Mol. Pharmacol. 87, 18.
      Ramana Reddy, M.V., et al. 2011. J. Med. Chem. 54, 6254.
      Gumireddy, K., et al. 2005. Cancer Cell 7, 275.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision20-November-2015 JSW
      SynonymsSodium (E)-2-(2-methoxy-5-((2,4,6-trimethoxystyrylsulfonyl)methyl)phenylamino)acetate, ON01910, Na, Estybon
      DescriptionA cell-permeable, nontoxic benzylstyrylsulfone based compound with anti-tumor and radiosensitizing properties. Potently suppresses PI 3-K/Akt/mTOR signaling pathway and activates Cdc25C phosphatases. Acts as an allosteric, substrate-competitive, and reversible inhibitor of multiple protein kinases (IC50 = 32, 42, 182, 18 and 155 nM against Bcr-Abl, Flt1, Fyn, PDGFR, and Src, respectively). Induces DNA damage and blocks microtubule formation. Also shown to cause mitotic arrest and apoptosis in multiple types of cancer cells (GI50 = 30 - 200 nM) and blocks cell cycle at G2/M phase. Effective against several multi-drug resistance tumor cells (IC50 = 50-100 nM). Suppresses the growth of BT20 tumor xenografts in mice and improves their survival rate (200 mg/kg, i.v. Q2D X 20 schedule). However, it displays limited oral bioavailability.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number592542-60-4
      Chemical formulaC₂₁H₂₄NNaO₈S
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesLu, T., et al. 2015. Mol. Pharmacol. 87, 18.
      Ramana Reddy, M.V., et al. 2011. J. Med. Chem. 54, 6254.
      Gumireddy, K., et al. 2005. Cancer Cell 7, 275.