Bioactivity | Antitumor agent-171 (Compound 35) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 1.61 μM. Antitumor agent-171 exhibits high affinity to β-catenin with Kd of 0.63 μM. Antitumor agent-171 inhibits the gene expression of axin2 with IC50 of 0.84 μM. Antitumor agent-171 inhibits cell viability of HCT116 with IC50 of 4.39 μM. Antitumor agent-171 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models[1]. |
Target | Kd: 0.63 μM (β-catenin);IC50: 1.61 μM (β-catenin/BCL9 interaction) |
CAS | 3003004-76-7 |
Formula | C35H45N7O5 |
Molar Mass | 643.78 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zhu W, et al., Discovery of Novel 1-Phenylpiperidine Urea-Containing Derivatives Inhibiting β-Catenin/BCL9 Interaction and Exerting Antitumor Efficacy through the Activation of Antigen Presentation of cDC1 Cells. J Med Chem. 2024 Jun 24. |