S80421 |
TH588 |
源叶(MedMol) | 98% |
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- 产品描述: TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
- 靶点: IC50: 5 nM (MTH1);DNA/RNASynthesis;MTH1
- 体外研究:
TH588 (2-10μM; 7-10 days) selectively and effectively kills U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM. Cell Viability Assay[1] Cell Line: U2OS, HeLa, MDA-MB-231, MCF-7, SW480, SW620, VH10, HDFn cells Concentration: 2, 4, 6, 8, 10 μM Incubation Time: 7-10 days Result: Selectively and effectively killed U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, but was less toxic to several primary or immortalized cells.
- 体内研究:
TH588 (30 mg/kg; s.c.; once daily for 35 days) reduces tumour growth in SW480 xenograft cancer model. Animal Model: 5-6 weeks female SCID mice (SW480 xenograft cancer model) Dosage: 30 mg/kg Administration: Subcutaneous injection; once daily for 35 days Result: Reduced tumour growth in SW480 xenograft cancer model.
- 参考文献:
1. Gad H, et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.388 ml 16.94 ml 33.879 ml 5 mM 0.678 ml 3.388 ml 6.776 ml 10 mM 0.339 ml 1.694 ml 3.388 ml 50 mM 0.068 ml 0.339 ml 0.678 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)