Danusertib
作者：齊岳
發布時間：2023-08-28
09:00:54
點擊數：
產品名稱：Danusertib
產品描述：
| 產品描述 | Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed. |
| 靶點活性 | TrkA:31 nM, Aurora A:13 nM, Abl:25 nM, FGFR1:47 nM, RET:31 nM |
| 體外活性 | Danusertib顯著抑制K562細胞的增殖,并在10天的治療期間抑制腫瘤的生長.給予HL-60異種移植大鼠25 mg/kg Danusertib（b.d.i.v.）導致75％的腫瘤生長被抑制,并且在一只動物中完全消退. |
| 體內活性 | 在細胞測定中,在用Danusertib處理野生型和p53缺陷型MEF后,野生型細胞在有絲分裂（4N）中停滯,持續48小時,而p53缺陷細胞不會在4N DNA階段停滯,持續有絲分裂,DNA變為>8N。Danusertib處理導致p53蛋白水平的上升和p21蛋白的增多,已知p53在轉錄水平上調節p21蛋白。Danusertib抑制其他激酶如FGFR1,Abl,Ret和Trka的活性,IC50分別為47 nM,25 nM,31 nM和31 nM。 |
| 激酶實驗 | Biochemical kinase Assays: The Km values for ATP and the specific substrate are initially determined, and each assay is then run at optimized ATP (2Km) and substrate (5Km) concentrations. This setting enabled direct comparison of IC50 values of Danusertib across the applied kinase selectivity screening panel for the evaluation of the selectivity profile. |
| 細胞實驗 | For short-term expansion assays, 1 × 103 CD34+ cells are plated in triplicates in 96-well plates containing 100 μL of serum-free medium per well supplemented with human stem-cell factor (100 ng/mL), human Flt-3 Ligand (100 ng/mL), human thrombopoietin (50 ng/mL), human interleukin-3 and -6 (IL-3 and IL-6, respectively, both 20 ng/mL), and granulocyte colony-stimulating factor (20 ng/mL) along with Danusertib at the indicated concentrations. After 5 days, an additional 100 μL of cytokine and Danusertib containing medium are added. Cell numbers within each individual well are estimated on days 3, 6, and 9 or on days 3, 6, and 12 for healthy donor samples. (Only for Reference) |
| 別名 | PHA-739358 |
| 分子量 | 474.55 |
| 分子式 | C26H30N6O3 |
| CAS No. | 827318-97-8 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 88 mg/mL (185.4 mM)
H2O: <1 mg/mL
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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