SBI-0206965 是一种强效, 选择性和细胞渗透性自噬激酶ULK1抑制剂, 抑制 ULK1 和 ULK2 激酶活性,IC50值分别为 108 nM 和 711 nM。
生物活性 | SBI-0206965 is a potent, selective and cell permeableautophagykinaseULK1inhibitor withIC50s of 108 nM forULK1kinase and 711 nM for the highly related kinaseULK2[1]. |
IC50& Target | ULK1 108 nM (IC50) | ULK2 711 nM (IC50) |
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体外研究 (In Vitro) | SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation[1]. SBI-0206965 (5-20 μM; 24 hours) attenuates the phosphorylation of Ser108 of the AMPK β1 subunit and increases the levels of cleaved Caspase 8 and PARP, markers of apoptosis[1].
Apoptosis Analysis[1] Cell Line: | A498 and ACHN cells (starvation medium (EBSS) treatment) | Concentration: | 5, 10 ,20 μM | Incubation Time: | 24 hours | Result: | Induced significant levels of apoptosis. |
Western Blot Analysis[1] Cell Line: | A498 and ACHN cells (EBSS treatment) | Concentration: | 5, 10, 20 μM | Incubation Time: | 24 hours | Result: | Attenuated the phosphorylation of Ser108 of the AMPK β1 subunit and increased the levels of cleaved Caspase 8 and PARP, markers of apoptosis. Autophagy was evaluated by analysis of LC3B and p62. |
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体内研究 (In Vivo) | SBI-0206965 (50 mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours[1].
Animal Model: | Six-week-old male BALB/c nude mice (A498 xenograft tumours)[1] | Dosage: | 50 mg/kg | Administration: | Intraperitoneal injection; once every three days for 37 days | Result: | Significantly suppressed tumour growth. |
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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 : ≥ 100 mg/mL(204.37 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.0437 mL | 10.2183 mL | 20.4365 mL | 5 mM | 0.4087 mL | 2.0437 mL | 4.0873 mL | 10 mM | 0.2044 mL | 1.0218 mL | 2.0437 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 (5.11 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.11 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。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.11 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。
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