product name TH287
Description: TH287 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 0.8 nM. TH287 selectively and effectively kill U2OS and other cancer cell lines with less toxic to several primary or immortalized cells, and induces oxidative DNA damage. 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.
References: Nature. 2014 Apr 10;508(7495):215-21; J Pharm Biomed Anal. 2015 Feb;104:1-11.
269.13
Formula
C11H10Cl2N4
CAS No.
1609960-30-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (196.9 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (37.2 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: TH287 selectively and effectively kill U2OS and other cancer cell lines with less toxic to several primary or immortalized cells, and induces oxidative DNA damage. Kinase Assay: Cell Assay: 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. |
|---|---|
| In Vivo | In C57Bl/6 mice, TH287 (5 mk/kg, i.p.) causes a peak time and maximum concentration of 0.5 h and 0.82μM. |
| Animal model | C57Bl/6 mice |
| Formulation & Dosage | Dissolved in 1% DMSO, 10% ethanol, 10% Chremophore EL and 10% Tween-80 and diluted with PBS; 5 mg/kg; i.p. injection. |
| References | Nature. 2014 Apr 10;508(7495):215-21; J Pharm Biomed Anal. 2015 Feb;104:1-11. |
