| CAS NO: | 1422253-38-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 询价 |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| 250mg | 询价 |
| Molecular Weight (MW) | 548.63 |
|---|---|
| Formula | C33H32N4O4 |
| CAS No. | 1422253-38-0; 847591-62-2; 1198780-38-9; 780757-88-2 (ICG001); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 100 mg/mL (182.3 mM) |
| Water: <1 mg/mL | |
| Ethanol: N/A | |
| Other info | Chemical Name: (6S,9aS)-N-benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxooctahydro-1H-pyrazino[1,2-a]pyrimidine-1-carboxamide SMILES Code: O=C(N(CC1)[C@](CN(CC2=C3C=CC=CC3=CC=C2)C([C@@H]4CC5=CC=C(O)C=C5)=O)([H])N4C1=O)NCC6=CC=CC=C6 |
| Synonyms | foscenvivint; PRI724; PRI-724; PRI 724; C-82 prodrug; ICG-001 analog; ICG001 isomer; ICG-001 isomer; ICG 001 isomer; ICG 001 analog; ICG001 analog; C 82 prodrug; C 82 prodrug; |
| In Vitro | In vitro activity: 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. Kinase Assay: The Dual-Luciferase Reporter (DLR) Assay System provides an efficient means of performing dual reporter assays. In the DLRTM Assay, the activities of firefly (Photinus pyralis) and Renilla (Renilla reniformis, also known as sea pansy) luciferases are measured sequentially from a single sample. The firefly luciferase reporter is measured first by adding Luciferase Assay Reagent II (LAR II) to generate a “glow-type” luminescent signal. After quantifying the firefly luminescence, this reaction is quenched, and the Renilla luciferase reaction is initiated by simultaneously adding Stop & Glo(R) Reagent to the same tube. The Stop & Glo(R) Reagent also produces a “glow-type” signal from the Renilla luciferase, which decays slowly over the course of the measurement. In the DLRTM Assay System, both reporters yield linear assays with subattomole (<10-18) sensitivities and no endogenous activity of either reporter in the experimental host cells. Furthermore, the integrated format of the DLRTM Assay provides rapid quantitation of both reporters either in transfected cells or in cell-free transcription/translation reactions. Cell Assay: The rat EMCs were treated with either ICG-001 or IQ1 and performed co-immunoprecipitation (co-IP) assays. Cells were treated with DMSO, ICG-001 or IQ1 for 24 hours. In the DMSO control treated cells, essentially all of the β-catenin was associated with CBP. Treatment with IQ1 had minimal effects on β-catenin coactivator usage. However, as anticipated, treatment with ICG-001 decreased the β-catenin/CBP interaction, while concomitantly increasing the β-catenin/p300 interaction. |
|---|---|
| In Vivo | 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. |
| Animal model | C57BL/6 and Balb/c mice |
| Formulation & Dosage | Dissolved in PBS; 300 mg/kg; i.p. administration |
| References | Transl Respir Med. 2014 Sep 11;2:8; Am J Cancer Res. 2015 Jul 15;5(8):2344-60. |
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