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506313 InSolution™ MPS1 Inhibitor, NMS-P715 - Calbiochem

A 5 mM (2 mg/592 µl) sterile-filtered solution of MPS1 Inhibitor, NMS-P715 in DMSO.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: N-(2,6-Diethylphenyl)-1-methyl-8-((4-(1-methylpiperidin-4-yl)carbamoyl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide, MPS1 Inhibitor, NMS-P715 InSolution

Primary Target: MPS1
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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      Empirical Formula
      C₃₅H₃₉F₃N₈O₃
      Description
      Overview

      This product has been discontinued.
      Catalogue Number506313
      Brand Family Calbiochem®
      SynonymsN-(2,6-Diethylphenyl)-1-methyl-8-((4-(1-methylpiperidin-4-yl)carbamoyl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide, MPS1 Inhibitor, NMS-P715 InSolution
      References
      ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
      Colombo, R., et al. 2011. Cancer Res. 70, 10255.
      Product Information
      FormLiquid
      FormulationA 5 mM (2 mg/592 µl) sterile-filtered solution of MPS1 Inhibitor, NMS-P715 (Cat. No. 475949) in DMSO.
      Hill FormulaC₃₅H₃₉F₃N₈O₃
      Chemical formulaC₃₅H₃₉F₃N₈O₃
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMPS1
      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 Dry Ice Only
      Toxicity Standard Handling
      Storage ≤ -70°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Avoid freeze/thaw Avoid freeze/thaw
      Do not freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. If necessary, slightly warm the vial. Use only fresh DMSO for further dilutions prior to use.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      506313 0

      Documentation

      InSolution™ MPS1 Inhibitor, NMS-P715 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Caldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
      Colombo, R., et al. 2011. Cancer Res. 70, 10255.
      Fiche technique

      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-July-2014 JSW
      SynonymsN-(2,6-Diethylphenyl)-1-methyl-8-((4-(1-methylpiperidin-4-yl)carbamoyl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide, MPS1 Inhibitor, NMS-P715 InSolution
      DescriptionAn 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.
      FormLiquid
      FormulationA 5 mM (2 mg/592 µl) sterile-filtered solution of MPS1 Inhibitor, NMS-P715 (Cat. No. 475949) in DMSO.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₅H₃₉F₃N₈O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      Storage Protect from light
      Avoid freeze/thaw
      ≤ -70°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. If necessary, slightly warm the vial. Use only fresh DMSO for further dilutions prior to use.
      Toxicity Standard Handling
      ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
      Colombo, R., et al. 2011. Cancer Res. 70, 10255.