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TH588

Catalog No.GC12716

MTH1 inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

TH588 Chemical Structure

Cas No.: 1609960-31-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$41.00
In stock
5mg
$41.00
In stock
25mg
$95.00
In stock
50mg
$163.00
In stock
100mg
$306.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Background

TH588 is a potent and selective MTH1 inhibitor (IC50 = 5 nM).

MTH1 (human MutT homolog 1) is an antimutagenic purine nucleoside triphosphatase that sanitize oxidized nucleotide pools. It’s a new cancer therapeutic target as it protects the cancer cell from DNA damages such as oxidative stress-induced cell dysfunction or death.

In U2OS and other cancer cell lines, TH588 treatment selectively and effectively kill cancer cells with less toxic to some primary or immortalized cells. U2OS cells treated with TH588 shows increase of 8-oxodG in DNA. The MTH1 inhibitor TH588 induces DNA damage and activates an ATM-p53-mediated death response and DNA repair in U2OS cells. [1]

Mice were transplanted with BRAFV600E-mutated melanoma, resistant to carboplatin, dacarbazine and vemurafenib. Ten of the tumor mice were randomized to receive TH588 once daily or vehicle control treatment. All TH588-treated mice had a reduced tumor growth rate, although the serum amount of TH588 decreased below IC50 concentrations during 24 hours treatment. [1]

Reference:
1.  Gad H, Koolmeister T, Jemth AS et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21.

Chemical Properties

Cas No. 1609960-31-7 SDF
Chemical Name (Z)-N-(6-(2,3-dichlorophenyl)-2-imino-2,3-dihydropyrimidin-4(1H)-ylidene)cyclopropanamine
Canonical SMILES ClC1=CC=CC(C(NC2=N)=C/C(N2)=N/C3CC3)=C1Cl
Formula C13H12Cl2N4 M.Wt 295.17
Solubility ≥ 7.38mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.3879 mL 16.9394 mL 33.8788 mL
5 mM 0.6776 mL 3.3879 mL 6.7758 mL
10 mM 0.3388 mL 1.6939 mL 3.3879 mL
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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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