Home DNA Damage/DNA Repair MTH1 inhibitor - NUDIX inhibitor TH588 For research use only.

TH588

TH588 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 5 nM. It has no relevant inhibition of any of the other tested proteins at 100 μM, although TH588 showed reasonable selectivity when tested on a much larger panel of 87 enzymes, GPCRs, kinases, ion channels and transporters at 10 μM.

TH588 Chemical Structure

TH588 Chemical Structure

CAS No. 1609960-31-7

Purity & Quality Control

TH588 Related Products

Biological Activity

Description TH588 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 5 nM. It has no relevant inhibition of any of the other tested proteins at 100 μM, although TH588 showed reasonable selectivity when tested on a much larger panel of 87 enzymes, GPCRs, kinases, ion channels and transporters at 10 μM.
Targets
NUDIX1 [1] MTH1 [1]
(cell-free assay)
5 nM
In vitro
In vitro TH588 selectively kill U2OS and other cancer cell lines with less toxic to several primary or immortalized cells. TH588 also induces DNA damage and triggers an ATM-p53-mediated death response and DNA repair in U2OS cells. [1]
In Vivo
In vivo In mice bearing SW480 colorectal or MCF7 breast tumor xenografts, TH588 (30 mg/kg s.c.) reduces tumor growth via MTH1 inhibition. In mice carrying patient with BRAFV600E mutated xenografts, TH588 (30 mg/kg s.c.) also causes a reduced tumor growth rate. [1]
Animal Research Animal Models SCID mice bearing SW480 xenografts or MCF-7 xenografts; NOD-SCID IL2Rγnull (NOG) mice bearing patient with BRAFV600E mutated xenografts
Dosages 30 mg/kg, once daily
Administration s.c.

Chemical Information & Solubility

Molecular Weight 295.17 Formula

C13H12Cl2N4
CAS No. 1609960-31-7 SDF Download TH588 SDF
Smiles C1CC1NC2=NC(=NC(=C2)C3=C(C(=CC=C3)Cl)Cl)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (199.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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