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• 產(chǎn)品描述： CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.

• 靶點： PI3Kα:6.8 nM (IC50);PI3Kβ:166 nM (IC50);PI3Kδ:240.3 nM (IC50);PI3Kγ:3020 nM (IC50);PI3K

• 體外研究：
  CNX-1351 is able to potently (EC50<100 nM) and specifically inhibit signaling in PI3Kα-dependent cancer cell lines, and this leads to a potent antiproliferative effect (GI50<100 nM). CNX-1351 inhibits PI3K signaling in SKOV3 cells, with potency (EC50 of 10-100 nM) similar to that of the pan-PI3K inhibitor. To investigate the functional consequence of inhibiting PI3Kα in cells, two cell lines with different PIK3CA activating mutations, SKOV3 ovarian cancer cells (H1047R) and MCF-7 breast cancer cells (E545K), are treated with CNX-1351 and growth is monitored. Both PIK3CA-driven cell lines are growth inhibited by exposure to CNX-1351 for 96 h (GI50 of 78 and 55 nM, respectively)

• 體內(nèi)研究：
  CNX-1351 inhibits p-AktSer473?in mouse spleens and bonds to PI3Kα in vivo. CNX-1351 is delivered into the intraperitoneal cavity of nude mice at 100 mg/kg once a day for 5 consecutive days (n=3 mice per group). Spleens are harvested from the mice at the indicated times after the last dose (1-24 h) and interrogated by immunoblot for P-AktSer473?or for PI3Kα occupancy. Inhibition of PI3K signaling is detected as a decrease in P-AktSer473?at 1 and 4 h after last dose

• 參考文獻：
  1. Nacht M, et al. Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. J Med Chem. 2013 Feb 14;56(3):712-21.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	1.743 ml	8.715 ml	17.43 ml
  5 mM	0.349 ml	1.743 ml	3.486 ml
  10 mM	0.174 ml	0.872 ml	1.743 ml
  50 mM	0.035 ml	0.174 ml	0.349 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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