506313 | InSolution™ MPS1 Inhibitor, NMS-P715 - Calbiochem

506313
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₅H₃₉F₃N₈O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.06313.0001
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service

          Glass bottle 2 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          Description
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          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 ≤ -70°C
          Hygroscopic
          Protect from light
          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.
          Toxicity Standard Handling
          ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
          Colombo, R., et al. 2011. Cancer Res. 70, 10255.