530916 MTH1 Inhibitor, TH588 - Calbiochem

530916
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₃H₁₂Cl₂N₄

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      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30916.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable, bioavailable diaminopyrimidine compound that acts as a potent, reversible, and active site targeting inhibitor of MTH1 (human MutT homolog 1; IC50 = 5 nM). The inhibition appears to be substrate independent in nature. Shown to selectively kill human osteosarcoma (U2OS) and other cancer cells, but display much reduced cytotoxicity towards several primary cells. Causes incorporation of oxidized dNTPs into cancer cells, leading to cytotoxic DNA damage, independent of their p53 status. However, it can also trigger ATM-p53-mediated death response and DNA repair in U2OS cells. Does not display any inhibitory activity against 87 enzymes, GPCRs, protein kinases, ion channels, and transporters even at 10 µM levels. Effectively suppresses MCF7 and SW480 tumor xenografts in mice (30 mg/kg, s.c., q.d.).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number530916
          Brand Family Calbiochem®
          SynonymsN⁴-Cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine, NUDT1 Inhibitor
          References
          ReferencesGad, H., et al. 2014. Nature 508, 215.
          Product Information
          FormLight beige powder
          Hill FormulaC₁₃H₁₂Cl₂N₄
          Chemical formulaC₁₃H₁₂Cl₂N₄
          ReversibleY
          Applications
          Biological Information
          Primary TargetMTH1
          Primary Target IC<sub>50</sub>5 nM
          Purity≥97% 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 freee (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          MTH1 Inhibitor, TH588 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Gad, H., et al. 2014. Nature 508, 215.
          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.

          Revision02-July-2014 JSW
          SynonymsN⁴-Cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine, NUDT1 Inhibitor
          DescriptionA cell-permeable, bioavailable diaminopyrimidine compound that acts as a potent, reversible, and active site targeting inhibitor of MTH1 (human MutT homolog 1; IC50 = 5 nM). The inhibition appears to be substrate independent in nature. Shown to selectively kill human osteosarcoma (U2OS) and other cancer cells, but display much reduced cytotoxicity towards several primary cells. Causes incorporation of oxidized dNTPs into cancer cells, leading to cytotoxic DNA damage, independent of their p53 status. However, it can also trigger ATM-p53-mediated death response and DNA repair in U2OS cells. Does not display any inhibitory activity against 87 enzymes, GPCRs, protein kinases, ion channels, and transporters even at 10 µM levels. Effectively suppresses MCF7 and SW480 tumor xenografts in mice (30 mg/kg, s.c., q.d.).
          FormLight beige powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₃H₁₂Cl₂N₄
          Purity≥97% by HPLC
          SolubilityDMSO (25 mg/ml). Not soluble in water.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freee (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesGad, H., et al. 2014. Nature 508, 215.