GSK2879552 是一种可口服的,不可逆的LSD1/ KDM1A抑制剂,具有抗肿瘤活性。
生物活性 | GSK2879552 an orally active, selective and irreversible inhibitor oflysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity[1][2]. |
体外研究 (In Vitro) | GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells[1].
Cell Proliferation Assay[2]. Cell Line: | 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines. | Concentration: | 0-10000 nM. | Incubation Time: | 6 days. | Result: | Inhibited cell proliferation. |
RT-PCR[1]. Cell Line: | Resistant HCC cells (PLC/PRF/5 and Huh7). | Concentration: | 0, 1, 2 μM. | Incubation Time: | 24 h. | Result: | Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9,
Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4. |
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体内研究 (In Vivo) | GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice[2].
Animal Model: | NCI-H526 and NCI-H1417 xenografts[2]. | Dosage: | 1.5 mg/kg. | Administration: | PO daily for 25-35 days. | Result: | There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(137.18 mM;Need ultrasonic) 配制储备液 1 mM | 2.7436 mL | 13.7182 mL | 27.4363 mL | 5 mM | 0.5487 mL | 2.7436 mL | 5.4873 mL | 10 mM | 0.2744 mL | 1.3718 mL | 2.7436 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: ≥ 2.75 mg/mL (7.54 mM); Clear solution
此方案可获得 ≥ 2.75 mg/mL (7.54 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 27.5 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.75 mg/mL (7.54 mM); Clear solution
此方案可获得 ≥ 2.75 mg/mL (7.54 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 27.5 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.75 mg/mL (7.54 mM); Clear solution
此方案可获得 ≥ 2.75 mg/mL (7.54 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 27.5 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。
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