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GSK-3685032
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK-3685032图片
CAS NO:2170137-61-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversibleDNMT1-selective inhibitor, with anIC50of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, andcancercell growth inhibition[1].

IC50& Target

DNMT1[1]

体外研究
(In Vitro)

GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC50value of 0.64 μM[1].
GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC50throughout a 6 d time course[1].
GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription[1].
GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression[1].
GSK3685032 induces DNA hypomethylation and gene activation[1].

Cell Proliferation Assay[1]

Cell 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 IC50value of 0.64 μM.

Cell Proliferation Assay[1]

Cell Line:MV4-11 cells
Concentration:0.1-1000 nM
Incubation Time:1-6 days
Result:Exhibited growth inhibition after 3 days, with decreasing growth IC50throughout a 6 d time course.

RT-PCR[1]

Cell 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 Analysis[1]

Cell Line:GDM-1 cells
Concentration:3.2-10,000 nM
Incubation Time:2 days
Result:Inhibited DNMT1 protein expression
体内研究
(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[1].

Summary of mouse pharmacokinetic parameters for GSK-3685032[1]

Dose,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-Foxn1mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc1NCrCrl mice, 8-11 weeks of age)[1]
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 ℃)
Administration:Subcutaneous injection, twice daily for 4 weeks
Result:Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.
分子量

420.53

性状

Solid

Formula

C22H24N6OS

CAS 号

2170137-61-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL(59.45 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3780 mL11.8898 mL23.7795 mL
5 mM0.4756 mL2.3780 mL4.7559 mL
10 mM0.2378 mL1.1890 mL2.3780 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (5.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (5.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (5.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.94 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。