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TH287

Catalog No.
B5849
MTH1 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$60.00
In stock
5mg
$70.00
In stock
10mg
$90.00
In stock
100mg
$470.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

TH287 is a potent MTH1 inhibitor with IC50 of 0.8±0.1 nM. [1]

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, TH287 treatment selectively and effectively kill cancer cells with less toxic to some primary or immortalized cells. U2OS cells treated with TH287 shows increase of 8-oxodG in DNA. The MTH1 inhibitor TH287 induces DNA damage and activates an ATM-p53-mediated death response and DNA repair in U2OS cells. [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

Physical AppearanceA solid
StorageStore at -20°C
M.Wt269.13
Cas No.1609960-30-6
FormulaC11H10Cl2N4
Solubility≥55.6mg/mL in DMSO
Chemical Name6-(2,3-dichlorophenyl)-N4-methylpyrimidine-2,4-diamine
SDFDownload SDF
Canonical SMILESClC1=C(Cl)C(C2=CC(NC)=NC(N)=N2)=CC=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control