• 产品描述： Nedisertib (M3814, Peposertib, MSC2490484A) 是一种口服可利用的、高效且选择性的 DNA activated protein kinase (DNA-PK) 的抑制剂，其IC50值小于3 nM

• 靶点： DNA-PK(Cell-free assay):3 nM

• 体外研究：
  M3814 potently inhibits DNA-PK catalytic activity and sensitizes multiple cancer cell lines to ionizing radiation (IR) and DSB-inducing agents. Inhibition of DNA-PK autophosphorylation in cancer cells leads to an increased number of persistent DSBs

• 体内研究：
  Inhibition of DNA-PK autophosphorylation in xenograft tumors leads to an increased number of persistent DSBs. Oral administration of M3814 to two xenograft models of human cancer, using a clinically established 6-week fractionated radiation schedule, strongly potentiates the antitumor activity of IR and lead to complete tumor regression at nontoxic doses

• 细胞实验： Cell lines: 92 cancer cell lines and resting peripheral blood mononuclear cells (PBMCs) Concentrations: 5 μmol/L–5 nmol/L Incubation Time: 120 h Method: Radiosensitization of 92 cancer cell lines and resting peripheral blood mononuclear cells (PBMCs) by M3814 is performed at Oncolead. Cell viability is determined with 3 Gy IR, M3814 (5 μmol/L–5 nmol/L), and a combination of 3 Gy IR and M3814 (5 μmol/L–5 nmol/L). Treated cells are incubated for 120 hours, fixed, stained with sulforhodamine B, and quantified colorimetrically.

• 动物实验： Animal Models: 7- to 9-week-old female NMRI (nu/nu) mice Dosages: 5 mg/kg, 25 mg/kg, 100 mg/kg Administration: Oral gavage

• 参考文献：
  1. Thomas Fuchss, et al. WO2014183850A1. 2. Frank T Zenke, et al. Pharmacologic Inhibitor of DNA-PK, M3814, Potentiates Radiotherapy and Regresses Human Tumors in Mouse Models. Mol Cancer Ther. 2020 May;19(5):1091-1101.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.075 ml	10.375 ml	20.751 ml
  5 mM	0.415 ml	2.075 ml	4.15 ml
  10 mM	0.208 ml	1.038 ml	2.075 ml
  50 mM	0.042 ml	0.208 ml	0.415 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。

输入产品批号：

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 *