496265 | Oncrasin-1 - CAS 75629-57-1 - Calbiochem

496265
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₁₆H₁₂ClNO75629-57-1

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      496265-25MG
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          Plastic ampoule 25 mg
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          Description
          OverviewA cell-permeable indolecarboxaldehyde compound that selectively induces apoptosis in cells harboring mutant K-Ras both in vitro (IC50 = 0.11, 0.25, 1.0, 1.58, and 4.81 µM in H2887, H460, H2122, A549, and T29Kt1 cultures, respectively) and in vivo (75% suppression of H460-derived tumor growth in mice; 100 mg/kg via daily i.p.), while exhibiting little or much reduced potency toward cells with wild-type Ras or mutant N-Ras (IC50 ≥31 µM). Oncrasin-1 treatment is shown to induce PKCι aggregation with splicing factors in the nucleus and dissociation between PKCι and CDK9/Cyclin T1 in K-Ras mutant cultures, resulting in decreased RNA polymerase II phosphorylation and a suppression of RNA processing in general. Oncrasin-1-induced cell death requires the presence of both mutant K-Ras and PKCι, siRNA-mediated knockdown of either enzyme is demonstrated to abolish its cytotoxicity in H460 and T29Kt1 cultures.
          Catalogue Number496265
          Brand Family Calbiochem®
          Synonyms1-((4-Chlorobenzyl)-1H-indole-3-carboxaldehyde, Oncogenic Ras Tumor-Inhibiting compound 1
          References
          ReferencesGuo, W., et al. 2009. Mol. Cancer Ther. 8, 441.
          Guo, W., et al. 2008. Cancer Res. 68, 7403.
          Product Information
          CAS number75629-57-1
          FormOff-white to light pink solid
          Hill FormulaC₁₆H₁₂ClNO
          Chemical formulaC₁₆H₁₂ClNO
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥95% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          R PhraseR: 36/38

          Irritating to eyes and skin.
          S PhraseS: 26-36-45

          In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
          Wear suitable protective clothing.
          In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Irritant
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          496265

          References

          Reference overview
          Guo, W., et al. 2009. Mol. Cancer Ther. 8, 441.
          Guo, W., et al. 2008. Cancer Res. 68, 7403.
          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.

          Revision11-October-2016 JSW
          Synonyms1-((4-Chlorobenzyl)-1H-indole-3-carboxaldehyde, Oncogenic Ras Tumor-Inhibiting compound 1
          DescriptionA cell-permeable indolecarboxaldehyde compound that selectively induces apoptosis in cells harboring mutant K-Ras both in vitro (IC50 = 0.11, 0.25, 1.0, 1.58, and 4.81 µM in H2887, H460, H2122, A549, and T29Kt1 cultures, respectively) and in vivo (75% suppression of H460-derived tumor growth in mice; 100 mg/kg via daily i.p.), while exhibiting little or much reduced potency toward cells with wild-type Ras or mutant N-Ras (IC50 ≥31 µM). Oncrasin-1 treatment is shown to induce PKCι aggregation with splicing factors in the nucleus and dissociation between PKCι and CDK9/Cyclin T1 in K-Ras mutant cultures, resulting in decreased RNA polymerase II phosphorylation and a suppression of RNA processing in general. Oncrasin-1-induced cell death requires the presence of both mutant K-Ras and PKCι, siRNA-mediated knockdown of either enzyme is demonstrated to abolish its cytotoxicity in H460 and T29Kt1 cultures.
          FormOff-white to light pink solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number75629-57-1
          Chemical formulaC₁₆H₁₂ClNO
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO or Ethanol
          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 Irritant
          ReferencesGuo, W., et al. 2009. Mol. Cancer Ther. 8, 441.
          Guo, W., et al. 2008. Cancer Res. 68, 7403.