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TH588MTH1 inhibitor

TH588

Catalog No. B5845
Size Price Stock Qty
5mg $60.00 In stock
25mg $140.00 In stock
50mg $240.00 In stock
100mg $440.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TH588

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Chemical Properties

Cas No. 1609960-31-7 SDF Download 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 Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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.