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• 產(chǎn)品描述： NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM)

• 靶點(diǎn)： IC50: 0.21 μM (Cdc25B2);Phosphatase

• 體外研究：
  NSC 663284 (3-100μM; 48 hours) has a mean IC50 value in the NCI 60 Cell human tumor panel of 1.5 ± 0.6 μM, has IC50 values of 0.2 μM in human breast cancer MDA-MB-435 and MDA-N cells, has an IC50 value of 1.7 μM in human breast MCF-7 cells in culture. NSC 663284 has relative IC50 values for Cdc25B2 (IC50=0.21 μM) are 20- and 450-fold lower than for VHR (IC50=4.0 μM) or PTP1B (IC50>4.0 μM), respectively

• 體內(nèi)研究：
  NSC 663284 (intravenous injection; 2, 3, and 5mg/kg) inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. After a single dose of 5 mg/kg, NSC 663284 is not detectable in plasma or tissues beyond 5 min. Following NSC 663284 treatment of tumor-bearing SCID mice, reduces glutathione concentrations in HT29 tumor are decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in liver and kidneys

• 參考文獻(xiàn)：
  1. Lazo JS, et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem. 2001 Nov 22;44(24):4042-9. 2. Coussens NP, et al. High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2. J Biol Chem. 2018 Aug 31;293(35):13750-13765. 3. Guo J, et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). Anticancer Res. 2007 Sep-Oct;27(5A):3067-73.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	3.108 ml	15.54 ml	31.079 ml
  5 mM	0.622 ml	3.108 ml	6.216 ml
  10 mM	0.311 ml	1.554 ml	3.108 ml
  50 mM	0.062 ml	0.311 ml	0.622 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(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)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(guān)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 *