产品描述: Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM. |
靶点:
ATR(Cell-free assay):7 nM;ATM/ATR |
体外研究:
BAY-1895344 inhibits tumor cell growth and viability and exhibits potent antiproliferative activity in a broad spectrum of human tumor cell lines |
体内研究:
BAY 1895344 exhibits strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies. |
细胞实验:
Cell lines: HT-29 cells, M059J cells, 38 cancer cell lines Concentrations: 3–300 nM Incubation Time: 72 to 96 hours Method: The antiproliferative activity of BAY 1895344 is evaluated against a panel of 38 cancer cell lines. Cell proliferation is measured after 72 to 96 hours of exposure to BAY1895344. Cell viability is determined using crystal violet staining or the CellTiter-Glo Cell Viability Assay. |
动物实验:
Animal Models: female SCID beige mice, female C.B-17 SCID mice, male NMRI nude mice, female NMRI nude mice Dosages: 50 mg/kg Administration: Oral gavage |
参考文献:
1. Ulrich T. Luecking, et al. Cancer Res 2017;77(13 Suppl):Abstract nr 983. 2. Antje M Wengner, et al. Mol Cancer Ther. 2020 Jan;19(1):26-38. |
溶解性:
Soluble in DMSO、Ethanol |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.428 ml |
12.139 ml |
24.278 ml |
5 mM |
0.486 ml |
2.428 ml |
4.856 ml |
10 mM |
0.243 ml |
1.214 ml |
2.428 ml |
50 mM |
0.049 ml |
0.243 ml |
0.486 ml |
|
注意: |
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