Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PTC-209 hydrobromide (PTC-209 HBr) 是一种特定的BMI-1抑制剂,能不可逆转地损害结直肠癌起始细胞,也可损害肿瘤微环境,有抗骨髓瘤活性。它在 HEK293T 细胞系中的IC50为 0.5 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 517 | 5日内发货 | ||
5 mg | ¥ 849 | 5日内发货 | ||
100 mg | ¥ 6,960 | 6-8周 |
PTC-209 hydrobromide 的其他形式现货产品:
产品描述 | PTC-209 hydrobromide (PTC-209 HBr) is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs). |
靶点活性 | BMI1:0.5 μM |
体外活性 | PTC-209 inhibits both the UTR-mediated reporter expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 decreases colorectal tumor cell growth in a BMI-1-dependent way. In addition, PTC-209 impairs colorectal cancer-initiating cells (CICs) through irreversible growth inhibition. [1] |
体内活性 | PTC-209 (60 mg/kg/day, s.c.) effectively inhibits BMI-1 production in tumor tissue, and halts growth of preestablished tumors in mice bearing primary human colon cancer xenograft, human colon cancer cell lines LIM1215 or HCT116 xenografts. PTC-209 also reduces the frequency of functional colorectal CICs in vivo. [1] |
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 | PTC-209 HBr |
分子量 | 576.1 |
分子式 | C17H13Br2N5OS·HBr |
CAS No. | 1217022-63-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: <1 mg/mL
H2O: <1 mg/mL
DMSO: 93 mg/mL (161.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7358 mL | 8.679 mL | 17.3581 mL | 43.3952 mL |
5 mM | 0.3472 mL | 1.7358 mL | 3.4716 mL | 8.679 mL | |
10 mM | 0.1736 mL | 0.8679 mL | 1.7358 mL | 4.3395 mL | |
20 mM | 0.0868 mL | 0.434 mL | 0.8679 mL | 2.1698 mL | |
50 mM | 0.0347 mL | 0.1736 mL | 0.3472 mL | 0.8679 mL | |
100 mM | 0.0174 mL | 0.0868 mL | 0.1736 mL | 0.434 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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