PTC-209
作者：齊岳
發(fā)布時(shí)間：2023-09-11
09:05:00
點(diǎn)擊數(shù)：
產(chǎn)品名稱(chēng)：PTC-209
產(chǎn)品描述：
| 產(chǎn)品描述 | PTC-209 is a potent and selective BMI-1 inhibitor. |
| 靶點(diǎn)活性 | BMI-1:0.5 μM |
| 體外活性 | PTC-209能降低體內(nèi)功能性的結(jié)直腸*CICs的頻率.PTC-209（60 mg/kg/day,s.c.）有效地抑制組織中BMI-1的產(chǎn)生,并停止在具有原代人結(jié)腸*異種移植物,人結(jié)腸*細(xì)胞系LIM1215或HCT116異種移植物的小鼠中預(yù)先建立的的生長(zhǎng). |
| 體內(nèi)活性 | PTC-209通過(guò)不可逆的生長(zhǎng)抑制破壞結(jié)腸直腸*起始細(xì)胞（CIC）。PTC-209抑制人結(jié)腸直腸HCT116和人纖維肉瘤HT1080細(xì)胞中UTR介導(dǎo)的報(bào)道基因表達(dá)和內(nèi)源性BMI-1表達(dá)。PTC-209以BMI-1依賴(lài)性減少直腸細(xì)胞的生長(zhǎng)。 |
| 激酶實(shí)驗(yàn) | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 別名 | PTC209, PTC 209 |
| 分子量 | 495.19 |
| 分子式 | C17H13Br2N5OS |
| CAS No. | 315704-66-6 |
存儲(chǔ)
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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