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• 产品描述： Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively

• 靶点： mTORC1:30 nM (IC50);mTORC2:58 nM (IC50);mTOR:8 nM (IC50);p110δ:100 nM (IC50);DNA-PK:410 nM (IC50);PDGFR:410 nM (IC50);p110α:2 μM (IC50);p110β:2.2 μM (IC50);p110γ:1.3 μM (IC50);Abl:3.6 μM (IC50);Hck:1.2 μM (IC50);Scr:1.4 μM (IC50);Scr(T338I):5.1 μM (IC50);VEGFR2:1.5 μM (IC50);EGFR:4.4 μM (IC50);EphB4:3.4 μM (IC50);Autophagy;Mitophagy;Apoptosis;Mitophagy;PI3K;mTOR;Autophagy

• 体内研究：
  In fat and liver, Torkinib (PP 242) is able to completely inhibit the phosphorylation of Akt at S473 and T308, consistent with its effect on these phosphorylation sites observed in cell culture. Surprisingly, Torkinib (PP 242) is only partially able to inhibit the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite it's ability to fully inhibit the phosphorylation of 4EBP1 and S6. These results will be confirmed by in vivo dose-response experiments, but, consistent with the partial effect of Torkinib (PP 242) on pAkt in skeletal muscle, a muscle-specific knockout of the integral mTORC2 component rictor resulted in only a partial loss of Akt phosphorylation at S473. These results suggest that a kinase other than mTOR, such as DNA-PK, may contribute to phosphorylation of Akt in muscle

• 参考文献：
  1. Apsel B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. 2. Feldman ME, et al. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 2009 Feb 10;7(2):e38.

• 溶解性： DMSO  :  50  mg/mL  (162.16  mM;  Need  ultrasonic)

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.243 ml	16.216 ml	32.432 ml
  5 mM	0.649 ml	3.243 ml	6.486 ml
  10 mM	0.324 ml	1.622 ml	3.243 ml
  50 mM	0.065 ml	0.324 ml	0.649 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 *