5.30916
MTH1 Inhibitor, TH588
Synonym(s):
MTH1 Inhibitor, TH588, N⁴-Cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine, NUDT1 Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C13H12Cl2N4
CAS Number:
Molecular Weight:
295.17
UNSPSC Code:
12352200
assay
≥97% (HPLC)
form
powder
potency
5 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light beige
solubility
DMSO: 25 mg/mL
water: insoluble
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MTH1
MTH1
Reversible: yes
Disclaimer
Toxicity: Standard Handling (A)
General description
A 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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Other Notes
Gad, H., et al. 2014. Nature508, 215.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freee (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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