PTC-209
作者：齐岳
发布时间：2023-09-11
09:05:00
点击数：
产品名称：PTC-209
产品描述：
| 产品描述 | PTC-209 is a potent and selective BMI-1 inhibitor. |
| 靶点活性 | BMI-1:0.5 μM |
| 体外活性 | PTC-209能降低体内功能性的结直肠癌CICs的频率.PTC-209（60 mg/kg/day,s.c.）有效地抑制肿瘤组织中BMI-1的产生,并停止在具有原代人结肠癌异种移植物,人结肠癌细胞系LIM1215或HCT116异种移植物的小鼠中预先建立的肿瘤的生长. |
| 体内活性 | PTC-209通过不可逆的生长抑制破坏结肠直肠癌起始细胞（CIC）。PTC-209抑制人结肠直肠HCT116和人纤维肉瘤HT1080肿瘤细胞中UTR介导的报道基因表达和内源性BMI-1表达。PTC-209以BMI-1依赖性减少直肠肿瘤细胞的生长。 |
| 激酶实验 | Untranslated region-mediated luciferase reporter expression: HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control. |
| 细胞实验 | To determine whether pretreatment with the inhibitor affects tumor cell growth, cells are plated with the inhibitor for 4 d in vitro and plated in limiting doses in vitro without adding further inhibitor. Trypan blue exclusion is used to count viable cells. The in vitro sphere-initiating cell frequency is calculated after inhibitor treatment by evaluating the number of wells containing spheres. For the experiments where LDAs are set up following recovery of PTC-209 treated cells, 6-well plates were seeded with 1E6 cells per well and incubated overnight. Cells are subsequently treated for 4 d in triplicate with either DMSO vehicle or PTC-209 (0.01, 0.1, 1 and 10 μM). Drug treatments are washed off and 4 mL fresh suspension medium added to all wells. To assess cell viability following the 4 d treatment window, cells are trypsinized and counted at 0, 24, 72 and 120 h after removal of the drug. Long-lasting effects of the drug treatment on sphere-forming ability are assessed by plating LDAs (50,000, 10,000, 1,000,100, 10 and 1 cell per well) using the cells obtained 120 h after the 4-d drug treatment.(Only for Reference) |
| 别名 | PTC209, PTC 209 |
| 分子量 | 495.19 |
| 分子式 | C17H13Br2N5OS |
| CAS No. | 315704-66-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 9.9 mg/mL (20 mM)
DMSO: 49.5 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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