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Product Details

TH588 | MTH1/NUDT1 inhibitor

TH588 (1609960-31-7) is a first-in-class nudix hydrolase family inhibitor.1 MTH1/NUDT1 is a family member that “sanitizes” oxidized deoxynucleotide triphosphates (dNTP) preventing their incorporation into DNA and thus avoiding DNA damage and cell death.  TH588 inhibits MTH1/NUDT1 (IC50 = 5 nM) leading to cell death in several cancer cell lines while not affecting normal cells.  Active in vitro and in vivo.  Recent evidence has raised doubts about the cancer-killing ability of MTH1 inhibition.2,3

References/Citations

1) Gad et al. (2014), MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool; Nature, 508 215
2) Petrocchi et al. (2016) Identification of potent and selective MTH1 inhibitors; Bioorg. Med. Chem. Lett., 26 1503
3) Kettle et al. (2016), Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival; J. Med. Chem., 59 2346

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Catalog#  10-4602

$55.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1609960-31-7 (free base)
Catalog Number:
10-4602
Activity:
MTH1/NUDT1 inhibitor
Chemical Name:
N4-Cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine hydrochloride
Molecular Weight:
331.63
Molecular Formula:
C13H12Cl2N4 &bul; HCl
Solubility:
Soluble in DMSO (up to 5 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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