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PTC-209

PTC-209

产品编号 T2345   CAS 315704-66-6
别名: PTC209, PTC 209

PTC-209 是特定的BMI-1抑制剂,不可逆转地损害结直肠癌起始细胞,在 HEK293T 细胞系中的IC50为 0.5 μM。它有抗骨髓瘤活性并损害肿瘤微环境。

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PTC-209 Chemical Structure
PTC-209, CAS 315704-66-6
规格 价格/CNY 货期 数量
2 mg ¥ 535 现货
5 mg ¥ 824 现货
10 mg ¥ 1,224 现货
50 mg ¥ 3,995 现货
100 mg ¥ 4,850 现货
200 mg ¥ 6,910 现货
其他形式的 PTC-209:
产品目录号及名称: PTC-209 (T2345)
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选择批次  
纯度: 99.60%
纯度: 99.52%
纯度: 99.43%
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生物活性
化学信息
存储 & 溶解度
参考文献
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 1 year

溶解度

Ethanol: 9.9 mg/mL (20 mM)

DMSO: 49.5 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.0194 mL 10.0971 mL 20.1943 mL 50.4857 mL
5 mM 0.4039 mL 2.0194 mL 4.0389 mL 10.0971 mL
10 mM 0.2019 mL 1.0097 mL 2.0194 mL 5.0486 mL
20 mM 0.101 mL 0.5049 mL 1.0097 mL 2.5243 mL
DMSO 50 mM 0.0404 mL 0.2019 mL 0.4039 mL 1.0097 mL
100 mM 0.0202 mL 0.101 mL 0.2019 mL 0.5049 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Kreso A, et al. Nat Med. 2014, 20(1), 29-36.

文献引用

1. Xu J, Zhang Y, Xu J, et al. Reversing tumor stemness via orally targeted nanoparticles achieves efficient colon cancer treatment. Biomaterials. 2019: 119247.
Sanguinarine chloride Gemcitabine GCN2iB Sorafenib Succinylsulfathiazole Quinacrine mustard hydrochloride Pictilisib Cisplatin

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抑制剂库 抗癌化合物库 DNA 损伤和修复分子库 已知活性化合物库 抗结直肠癌化合物库 表型筛选靶点鉴定库 自噬库 经典已知活性库 细胞周期化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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计算 重置

技术支持

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。

Keywords

PTC-209 315704-66-6 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair BMI-1 tumor cells inhibit anti-myeloma HEK293T cancer-initiating lung CICs breast PTC209 PTC 209 colon Inhibitor inhibitor

 

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