• 产品描述： Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).

• 靶点： Topoisomerase I:0.31 μM (IC50);Camptothecins;Topoisomerase

• 体外研究：
  Dxd shows obviously suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines with IC50s of 26.8, 25.4, and 6.7 ng/mL respectively, but with no such inhibition on MDA-MB-468 (IC50, >10,000 ng/mL)

• 体内研究：
  Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s of 1.43 nM-4.07 nM. In HER2 low-expressing ST565 and ST313 models has HER2 IHC 1+/FISH-negative expression

• 参考文献：
  1. Ogitani Y, et al. DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1. Clin Cancer Res. 2016 Oct 15;22(20):5097-5108.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.026 ml	10.132 ml	20.264 ml
  5 mM	0.405 ml	2.026 ml	4.053 ml
  10 mM	0.203 ml	1.013 ml	2.026 ml
  50 mM	0.041 ml	0.203 ml	0.405 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 *