TH588 (2-10μM; 7-10 days) selectively and efficiently eradicates U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells, displaying IC50 values of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, respectively[1].
体内研究
TH588 (30 mg/kg; sC.; once daily for 35 days) effectively reduces tumor growth in the SW480 xenograft cancer model[1].
体外研究
TH588 (2-10μM; 7-10 days) selectively and efficiently eradicates U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells, displaying IC50 values of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, respectively[1].
作用机制
TH588 inhibits MTH1 by forming hydrogen bonds with Phe72 and Met81 and π-π stacking with Phe72.
TH588 细胞实验
Cell Line
Concentration
Treated Time
Description
References
A431 cells
10 μM
24 hours
Evaluate the anticancer activity of TH588 on A431 cells, with an IC50 value of 25 μM
Sci Adv. 2020 Mar 4;6(10):eaaz0575.
HOS-MNNG cells
8 μM
24 hours
Evaluate the effect of TH588 on DNA damage in HOS-MNNG cells, results showed TH588 increased DNA strand breaks.
EBioMedicine. 2020 Mar;53:102704.
U2OS cells
2 μM and 8 μM
48 hours
Evaluate the effect of TH588 on clonogenicity of U2OS cells, results showed 2 μM and 8 μM TH588 reduced colony formation by 13% and 91% respectively.
EBioMedicine. 2020 Mar;53:102704.
HOS-MNNG cells
2 μM and 8 μM
48 hours
Evaluate the effect of TH588 on clonogenicity of HOS-MNNG cells, results showed 2 μM and 8 μM TH588 reduced colony formation by 53.4% and 91.5% respectively.
EBioMedicine. 2020 Mar;53:102704.
TH588 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
A431 tumor xenograft model
Intravenous injection
50 μM
Repeated every 5 days for 20 days
Evaluate the therapeutic effect of TH588 and Ce6 combined therapy on A431 tumor xenograft model, showing significant tumor volume reduction
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