For research use only. Not for therapeutic Use.
TH287 is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 could act as a chemotherapeutic agent for cancer research[1].
TH287 (1-10 μM; 24 h) selectively and effectively kills U2OS and other cancer cell lines, but is considerably less toxic to several primary or immortalized cells[1].
TH287 (5 mg/kg; i.p.) exhibits Cmax of 0.82 μM and tmax of 0.5 h in mice[2].
| Catalog Number | I002050 |
| CAS Number | 1609960-30-6 |
| Synonyms | 6-(2,3-dichlorophenyl)-4-N-methylpyrimidine-2,4-diamine |
| Molecular Formula | C11H10Cl2N4 |
| Purity | ≥95% |
| InChI | InChI=1S/C11H10Cl2N4/c1-15-9-5-8(16-11(14)17-9)6-3-2-4-7(12)10(6)13/h2-5H,1H3,(H3,14,15,16,17) |
| InChIKey | URWCXPXBBITYLR-UHFFFAOYSA-N |
| SMILES | CNC1=NC(=NC(=C1)C2=C(C(=CC=C2)Cl)Cl)N |
| Reference | [1]. Gad H, et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21. [2]. Saleh A, et, al. Development and validation of method for TH588 and TH287, potent MTH1 inhibitors and new anti-cancer agents, for pharmacokinetic studies in mice plasma. J Pharm Biomed Anal. 2015 Feb;104:1-11. |
