530916 MTH1 Inhibitor, TH588 - Calbiochem

530916
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₃H₁₂Cl₂N₄

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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
      Quality LevelMQ100
      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.