產品描述: VE-822 has been used in trials studying the treatment of Ovarian Neoplasms, Ovarian Serous Tumor, Adult Solid Neoplasm, Advanced Solid Tumor, and Advanced Solid Neoplasm, among others. |
靶點:
ATM/ATR |
體內研究:
80 nM VE-822單獨使用增加MiaPaCa-2和PSN-1細胞停留在G1期的比率。80 nM VE-822消除MiaPaCa-2和PSN-1細胞中富含XRT的G2/M期部分。VE-822單獨作用不大,而80 nM VE-822與XRT和/或gemcitabine聯用則增強PSN-1細胞中的早期和晚期細胞凋亡。VE-822增加對與pChk1 Ser345阻斷相關的DNA損傷劑的腫瘤應答。VE-822(80 nM)減弱ATR信號傳導途徑并降低腫瘤細胞對XRT和吉西他濱的應答的存活率。在正常細胞中,80 nM VE-822減弱ATR信號通路強度,但并沒有增強輻射和gemcitabine殺傷正常細胞的能力 |
細胞實驗:
VE-822 is dissolved in DMSO and stored, and then diluted with appropriate media before use. Gemcitabine (10 nM) is added 24 h pre-XRT and is replaced with fresh medium before addition of VE-822. PSN-1 cells are treated with VE-822 (80 nM) for 1 h before, through to 18 h after, XRT (6 Gy). Apoptosis is analyzed 48 h after XRT by flow cytometry using an Annexin V-FITC kit with Pl |
參考文獻:
1.Fokas E, et al. Cancer Treat Rev, 2013, pii: S0305-7372(13)00065-0. 2.Fokas E, et al. Cell Death Dis, 2012, 3, e441. 3.Konstantinopoulos P A , Cheng S C , Hendrickson A E W , et al. Berzosertib plus gemcitabine versus gemcitabine alone in platinum-resistant high-grade serous ovarian cancer: a multicentre, open-label, randomised, phase 2 trial[J]. The Lancet Oncology, 2020, 21(7). |
溶解性:
DMSO:34 mg/mL (73.3 mM) Ethanol:<1 mg/mL |
保存條件:
2-8℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
2.157 ml |
10.786 ml |
21.573 ml |
5 mM |
0.431 ml |
2.157 ml |
4.315 ml |
10 mM |
0.216 ml |
1.079 ml |
2.157 ml |
50 mM |
0.043 ml |
0.216 ml |
0.431 ml |
|
注意: |
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