产品
编 号：F741400
分子式：C22H24N6OS
分子量：420.53
分子式：C22H24N6OS
分子量：420.53
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2170137-61-6
产品详情
生物活性：
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
体内研究：
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-3685032Dose,RouteCmax(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,IV510324181209131.31.8
2 mg/kg,SC252921461NANA2.8
2 mg/kg,SC547315400513NANAND
Animal Model:MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc1NCrCrl mice, 8-11 weeks of age)
Dosage:1, 5, 15, 30, 45 mg/kg (10% captisol adjusted to pH 4.5-5 with 1 M acetic acid, stored for up to 1 week at 4 °C)
Administration:Subcutaneous injection, twice daily for 4 weeks
Result:Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.
体外研究：
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.
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
体内研究：
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-3685032Dose,RouteCmax(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,IV510324181209131.31.8
2 mg/kg,SC252921461NANA2.8
2 mg/kg,SC547315400513NANAND
Animal Model:MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc1NCrCrl mice, 8-11 weeks of age)
Dosage:1, 5, 15, 30, 45 mg/kg (10% captisol adjusted to pH 4.5-5 with 1 M acetic acid, stored for up to 1 week at 4 °C)
Administration:Subcutaneous injection, twice daily for 4 weeks
Result:Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.
体外研究：
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.
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