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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      5.33575.0001
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          Glass bottle 10 mg
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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
          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.