• 產(chǎn)品描述： AZD7648是DNA-PK的有效抑制劑，IC50為0.6 nM，其選擇性比對所檢測激酶庫中其他的396種激酶高100倍以上

• 靶點(diǎn)： DNA-PK(Cell-free assay):0.6 nM;DNA-PK

• 體外研究：
  AZD7648 inhibits IR-induced DNA-PK S2056 auto phosphoryalation with an IC50 = 92 nM in A549 non-small cell lung cancer (NSCLC) cells. In A549 cells, AZD7648 (≥1 μM) in combination with 2Gy IR for 48 hours leads to a significant accumulation of cells arrested in the G2/M of the cell cycle, a 4-fold increase in micronuclei formation, and 3-fold induction of γH2AX, pATM S1981 and 53BP1 foci formation compared with IR alone

• 體內(nèi)研究：
  AZD7648 is a potent and highly selective DNA-PK inhibitor, with good crystalline solubility, permeability and metabolic stability, good bioavailability and predictable pharmacokinetics in preclinical species, and potent knockdown of pRPA and regressions in murine xenograft models when combining with olaparib or radiation

• 細(xì)胞實驗： Cell lines: HeLa cells Concentrations: 10 μM Incubation Time: 1 h Method: Cells were treated with indicated concentration of drug for 1 h.

• 動物實驗： Animal Models: SCID mice Dosages: 4-100 mg/kg Administration: p.o.

• 參考文獻(xiàn)：
  1. Frederick W. Goldberg, et al. Abstract DDT01-02: Discovery and first structural disclosure of AZD7648: A potent and selective DNA-PK inhibitor. AACR Cancer Res. 2019, 79(13 Suppl):Abstract nr DDT01-02. 2. Jacqueline H. Fok, et al. Abstract 3512: AZD7648, a potent and selective inhibitor of DNA-PK, potentiates the activity of ionising radiation and doxorubicin in vitro and causes tumour regression in xenograft models. AACR Cancer Res. 2019, 79(13 Suppl):Abstract nr 3512. 3. Zhang H, et al. TDP1-independent pathways in the process and repair of TOP1-induced DNA damage. Nat Commun. 2022 Jul 22;13(1):4240. 4. Fok JHL, et al. TDP1-independent pathways in the process and repair of TOP1-induced DNA damage. Nat Commun. 2019 Nov 7;10(1):5065.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存條件： -20°C

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.629 ml	13.144 ml	26.288 ml
  5 mM	0.526 ml	2.629 ml	5.258 ml
  10 mM	0.263 ml	1.314 ml	2.629 ml
  50 mM	0.053 ml	0.263 ml	0.526 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：

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(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 *