Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ICG001 (PRI-724 isomer) 拮抗 Wnt/β-catenin/TCF 介导的转录,并特异性结合元件结合蛋白(CREB) 结合蛋白 (CBP),IC50 为 3 μM,但不是相关的转录共激活因子 p300。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 322 | 现货 | ||
5 mg | ¥ 762 | 现货 | ||
10 mg | ¥ 993 | 现货 | ||
25 mg | ¥ 2,090 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,690 | 现货 | ||
500 mg | ¥ 11,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 919 | 现货 |
产品描述 | ICG001 (PRI-724 isomer) antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. |
靶点活性 | CBP:3 μM |
体外活性 | PRI-724 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin. Treatment with PRI-724 selectively induces apoptosis in colon carcinoma cells but not in normal colonic epithelial cells and reduces in vitro growth of colon carcinoma cells[1][2]. |
体内活性 | PRI-724 exhibits antitumor activity in the mouse xenograft models of colon cancer. The initial results of the Phase I clinic trial of PRI-724 has been disclosed publically. The drug exhibits an acceptable toxicity profile with only one dose-limiting toxicity of grade 3 reversible hyperbilirubinaemia. An Open-Label dose-escalation phase I/II study of PRI-724 for patients with advanced myeloid malignancies is still ongoing[2]. |
细胞实验 | ICG-001 is dissolved in DMSO. To evaluate effects of ICG-001 on α-SMA and collagen type 1 expression, RLE-6TN cells are treated with TGF-β1 (0.25 ng/mL) in the presence or absence of ICG-001 (5.0 μM). After 24 h, cells are harvested and mRNA isolated for analysis by qPCR. RNA is reverse-transcribed using SuperScript reverse transcriptase. Quantitative PCR is performed with SYBR-Green PCR using Real-Time PCR System HT7900. The amplification protocol is set as follows: 95°C denaturation for 10 min followed by 40 cycles of 15-s denaturation at 95°C, 1 min of annealing/extension, and data collection at 60°C. |
分子量 | 548.63 |
分子式 | C33H32N4O4 |
CAS No. | 847591-62-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 54.9 mg/mL (100 mM)
Ethanol: 27.4 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.8227 mL | 9.1136 mL | 18.2272 mL | 45.5681 mL |
5 mM | 0.3645 mL | 1.8227 mL | 3.6454 mL | 9.1136 mL | |
10 mM | 0.1823 mL | 0.9114 mL | 1.8227 mL | 4.5568 mL | |
20 mM | 0.0911 mL | 0.4557 mL | 0.9114 mL | 2.2784 mL | |
50 mM | 0.0365 mL | 0.1823 mL | 0.3645 mL | 0.9114 mL | |
DMSO | 100 mM | 0.0182 mL | 0.0911 mL | 0.1823 mL | 0.4557 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。
ICG001 847591-62-2 Chromatin/Epigenetic Cytoskeletal Signaling Stem Cells Epigenetic Reader Domain Wnt/beta-catenin 780757-88-2 PRI 724 ICG 001 PRI724 ICG-001 Inhibitor inhibitor inhibit