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CAS No. : 2170137-61-6
MCE 国际站:GSK-3685032
产品活性:GSK-3685032 是一种非时间依赖、非共价、可逆的 DNMT1 选择性抑制剂,IC50=0.036 μM。GSK-3685032 诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。
研究领域:Epigenetics
作用靶点:DNA Methyltransferase
In Vitro: GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM.
GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course.
GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription.
GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression.
GSK3685032 induces DNA hypomethylation and gene activation.
In Vivo: GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models.
Summary of mouse pharmacokinetic parameters for GSK-3685032
Dose,Route | Cmax (ng/mL) | AUC0-8hr (h*ng/mL) | DNAUC (h*kg*ng/mL/mg) | Clearance (mL/min/kg) | Volumedss (L/kg) | T1/2 (h) |
2 mg/kg,IV | 5103 | 2418 | 1209 | 13 | 1.3 | 1.8 |
2 mg/kg,SC | 252 | 921 | 461 | NA | NA | 2.8 |
2 mg/kg,SC | 5473 | 15400 | 513 | NA | NA | ND |
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