• 产品描述： PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis

• 靶点： DNA-PK:2 nM (IC50);p110α:5.8 nM (IC50);p110γ:76 nM (IC50);p110δ:510 nM (IC50);p110β:1.3 μM (IC50);hsVPS34:2.6 μM (IC50);PI3KC2β:1 μM (IC50);PI3KC2α:10 μM (IC50);mTORC1:1 μM (IC50);mTORC2:10 μM (IC50);ATM:2.3 μM (IC50);ATR:21 μM (IC50);PI4KIIIβ:50 μM (IC50);Apoptosis; DNA-PK; PI3K

• 体外研究：
  PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC50s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively. PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC50 values of 1.2 and 1.3 μM, respectively. PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC50 of 78 nM. PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death. PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells. Cell Viability Assay Cell Line: Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1) Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM Incubation Time: 48 hours Result: Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment. Western Blot Analysis Cell Line: Overnight-starved CHO-IR cells Concentration: 1, 10, 100, 1000 nM Incubation Time: 5 minutes Result: Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner. PIK-75 potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabin

• 体内研究：
  PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice. Animal Model: Mice bearing tumors of MIA PaCa-2 Dosage: 2 mg/kg; or combination with Gemcitabine (20 mg/kg) Administration: Administered injection; 5 times per week. 25 days Result: Reduced the tumor growth and enhanced the antitumor effect.

• 参考文献：
  1. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. 2. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. 3. Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69.

• 溶解性： DMSO  (warmed  with  50ºC  water  bath)：  3  mg/mL  (6.14  mM)

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.211 ml	11.055 ml	22.11 ml
  5 mM	0.442 ml	2.211 ml	4.422 ml
  10 mM	0.221 ml	1.105 ml	2.211 ml
  50 mM	0.044 ml	0.221 ml	0.442 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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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 *