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• 产品描述： SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2

• 靶点： ULK1:108 nM (IC50);ULK2:711 nM (IC50);Apoptosis;Autophagy

• 体外研究：
  SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation. 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. Apoptosis Analysis 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 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.

• 体内研究：
  SBI-0206965 (50 mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours. Animal Model: Six-week-old male BALB/c nude mice (A498 xenograft tumours) Dosage: 50 mg/kg Administration:Intraperitoneal injection; once every three days for 37 days Result: Significantly suppressed tumour growth.

• 参考文献：
  1. Lu J, et al. Overexpression of ULK1 Represents a Potential Diagnostic Marker for Clear Cell RenalCarcinoma and the Antitumor Effects of SBI-0206965. EBioMedicine. 2018 Aug;34:85-93. 2. Egan DF, et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16;59(2):285-97.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.044 ml	10.218 ml	20.437 ml
  5 mM	0.409 ml	2.044 ml	4.087 ml
  10 mM	0.204 ml	1.022 ml	2.044 ml
  50 mM	0.041 ml	0.204 ml	0.409 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *