475949 MPS1 Inhibitor, NMS-P715 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₃₅H₃₉F₃N₈O₃

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475949-5MG
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      Description
      OverviewAn orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50 = 182 nM, Ki = 0.99 nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (< 10 µM), but not against other mitotic kinases including PLK1, CDK1, Aurora A, Aurora B, or the SAC kinase BUB1, in an in vitro kinase assay. It promotes massive SAC (spindle assembly checkpoint) override (EC50 = 65 nM) in nocodazole-arrested U20S cells and elicits a reduction in the G1 and G2/M phase of the cell cycle in A2780 ovarian cancer cells, similar to RNAi-mediated MPS1 silencing. In addition, it is shown to inactivate SAC, delocalize kinetochore components, and inhibit the proliferation of select cancer cell lines (IC50 ~ 1 µM), without marked activity among a panel of 127 normal cell lines. Also, it inhibits A2780 tumor xenograft growth in mice (90 mg/kg/day, o.s., in vivo) by 53% without marked body weight loss. Also available as a 5 mM solution in DMSO (Cat. No. 506313).
      Catalogue Number475949
      Brand Family Calbiochem®
      Synonyms(N-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide)
      References
      ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
      Colombo, R., et al. 2011. Cancer Res. 70, 10255.
      Product Information
      FormWhite powder
      Hill FormulaC₃₅H₃₉F₃N₈O₃
      Chemical formulaC₃₅H₃₉F₃N₈O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationMPS1 Inhibitor, NMS-P715, CAS 1202055-32-0, is an orally bioavailable, ATP-competitive, reversible, and time-dependent inhibitor of MPS1 (IC50 = 182 nM, Ki = 0.99 nM).
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      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

      MPS1 Inhibitor, NMS-P715 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      MPS1 Inhibitor, NMS-P715 - Calbiochem Certificates of Analysis

      TitleLot Number
      475949

      References

      Reference overview
      Caldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
      Colombo, R., et al. 2011. Cancer Res. 70, 10255.
      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.

      Revision08-June-2012 JSW
      Synonyms(N-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide)
      DescriptionAn orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50 = 182 nM, Ki>sub> = 0.99 nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (< 10 µM), but not against other mitotic kinases including PLK1, CDK1, Aurora A, Aurora B, or the SAC kinase BUB1, in an in vitro kinase assay. It promotes massive SAC (spindle assembly checkpoint) override (EC50 = 65 nM) in nocodazole-arrested U20S cells and elicits a reduction in the G1 and G2/M phase of the cell cycle in A2780 ovarian cancer cells, similar to RNAi-mediated MPS1 silencing. In addition, it is shown to inactivate SAC, delocalize kinetochore components, and inhibit the proliferation of select cancer cell lines (IC50 ~ 1 µM), without marked activity among a panel of 127 normal cell lines. Also, it inhibits A2780 tumor xenograft growth in mice (90 mg/kg/day, o.s., in vivo) by 53% without marked body weight loss.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₅H₃₉F₃N₈O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (10 mg/ml; clear, colorless solution)
      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
      ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
      Colombo, R., et al. 2011. Cancer Res. 70, 10255.