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ICG001
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ICG001图片
CAS NO:847591-62-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
PRI-724 isomer
PRI-724
产品介绍
ICG001 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。

产品描述

ICG-001 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.

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.

Cas No.

847591-62-2

分子式

C33H32N4O4

分子量

548.63

别名

PRI-724 isomer;PRI-724

储存和溶解度

DMSO:54.9 mg/mL (100 mM)
Ethanol:27.4 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years