计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1 -selective inhibitor, with an IC 50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition
In Vitro
GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC 50 value of 0.64 μM. GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: 15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells. Concentration: 0.01-100 μM Incubation Time: 6 days Result: Showed cell growth inhibition of majority cancer cell lines, with a median growth IC 50 value of 0.64 μM. Cell Proliferation AssayCell Line: MV4-11 cells Concentration: 0.1-1000 nM Incubation Time: 1-6 days Result: Exhibited growth inhibition after 3 days, with decreasing growth IC 50 throughout a 6 d time course. RT-PCRCell Line: MV4-11 cells Concentration: 10-10000 nM Incubation Time: 4 days Result: Dose-dependent increased of CXCL11, IFI27, HLA-DQA1 and MAGEA4 following treatment of MV4-11 cells. Western Blot AnalysisCell Line: GDM-1 cells Concentration: 3.2-10,000 nM Incubation Time: 2 days Result: Inhibited DNMT1 protein expression
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 C max (ng/mL) AUC 0-8hr (h*ng/mL) DNAUC (h*kg*ng/mL/mg) Clearance (mL/min/kg) Volume dss (L/kg) T 1/2 (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 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc 1NCrCrl 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.
Form:Solid
IC50& Target:DNMT1
规格
规格或纯度
≥99%
英文名称
GSK-3685032
生化机理
GSK-3685032 是一种非时间依赖性、非共价、一流的可逆 DNMT1 选择性抑制剂，IC 50 为 0.036 μM。GSK-3685032 可诱导强效的 DNA 甲基化缺失、转录激活和癌细胞生长抑制。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
420.53
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 25 mg/mL (59.45 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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