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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 106 | |
4 mg | In stock | $ 180 | |
8 mg | In stock | $ 252 | |
20 mg | In stock | $ 478 | |
40 mg | In stock | $ 721 |
Description | 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. |
Targets&IC50 | CBP:3 μM |
In vitro | 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. |
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. |
Synonyms | PRI-724 isomer, PRI-724 |
CAS No. | 847591-62-2 |
Chemical Formula | C33H32N4O4 |
Molecular Weight | 548.63 |
Solubility | Ethanol: 27.4 mg/mL (50 mM) DMSO: 54.9 mg/mL (100 mM) |
Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
bottom