| Chemical Properties | Back Directory | [Boiling point ]
651.3±65.0 °C(predicted) | [density ]
1.370±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
7.89±0.20(predicted) |
| Hazard Information | Back Directory | [Uses]
TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research[1]. | [in vivo]
TRIM24/BRPF1-IN-2 (compound 20l) (50 mg/kg, IP, once daily for 21 days) suppresses tumor growth (TGI = 53%) without exhibiting noticeable toxicity[1]. | Animal Model: | Mice (n = 5-7 per dose group, Four-week-old, male, non-obese diabetic server combined immune-deficiency (NOD SCID), 22Rv1 xenograft model)[1] | | Dosage: | 50 mg/kg | | Administration: | IP, once daily for 21 days | | Result: | Inhibited the progression of the tumors significantly (53% tumor growth inhibition) without body weight loss. |
| [IC 50]
BRPF1: 1.16 μM (IC50) | [References]
[1] Xiang Q, et al. Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors. Eur J Med Chem. 2022 Jun 5;236:114311. DOI:10.1016/j.ejmech.2022.114311 |
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