- SCH 51344
- TH588
- (S)-Crizotinib
| TH287MTH1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.68%
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Chemical structure
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| Cas No. | 1609960-30-6 | SDF | Download SDF |
| Chemical Name | 6-(2,3-dichlorophenyl)-N4-methylpyrimidine-2,4-diamine | ||
| Canonical SMILES | ClC1=C(Cl)C(C2=CC(NC)=NC(N)=N2)=CC=C1 | ||
| Formula | C11H10Cl2N4 | M.Wt | 269.13 |
| Solubility | ≥55.6mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
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.
