| Identification | Back Directory | [Name]
Research Grade Ipafricept (DHK29201) | [CAS]
1391727-24-4 | [Synonyms]
Ipafricept
Research Grade Ipafricept (DHK29201) |
| Hazard Information | Back Directory | [Uses]
Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer[1][2][3]. | [in vivo]
Ipafricept (10 mg/kg weekly or 25 mg/kg every 2 weeks, i.p., for 42 days) promotes tumor growth inhibition when combined with weekly Gemcitabine (HY-17026) (50 mg/kg or 5 mg/kg weekly) and Nab-paclitaxel (HY-P99974) (10 mg/kg weekly) in pancreatic cancer xenograft mouse models[2].
Ipafricept (45 mg/kg every 2 weeks, i.p., for 42 days) results in greater antitumor activity of WNT blockade and tumor growth inhibition in combination with Nab-paclitaxel (HY-P99974) (7.5 mg/kg every week) than Carboplatin (HY-17393) (30 mg/kg every week) in ovarian cancer xenograft mouse models[2].
Ipafricept (10 mg/kg, s.c., administered on day 0 and 3) competes with RL-QN15 for binding, reducing the interaction of RL-QN15 with FZD8, thereby counteracting its activation of the Wnt/β-catenin signaling pathway in mouse full-thickness skin injury models[3].
| Animal Model: | Pancreatic cancer xenograft mouse models[2] | | Dosage: | 10 mg/kg weekly or 25 mg/kg every 2 weeks | | Administration: | i.p., weekly or every 2 weeks for 42 days | | Result: | Markedly increased the antitumor activity in combination with Gemcitabine (HY-17026) and Nab-paclitaxel (HY-P99974) in pancreatic cancer xenograft mouse models. |
| Animal Model: | Ovarian cancer xenograft mouse models[2] | | Dosage: | 45 mg/kg every 2 weeks | | Administration: | i.p., every 2 weeks for 42 days | | Result: | Resulted in greater tumor growth inhibition in combination with Nab-paclitaxel (HY-P99974) than Carboplatin (HY-17393) in ovarian cancer xenograft mouse models. |
| Animal Model: | Mouse full-thickness skin injury models[3] | | Dosage: | 10 mg/kg | | Administration: | s.c., administered on day 0 and 3 | | Result: | Decreased the skin wound healing rate to less than 60% combined with RL-QN15 and inhibited RL-QN15-induced re-epithelialization in mouse full-thickness skin injury models. |
| [References]
[1] Jimeno A, et al. A First-in-Human Phase I Study of the Anticancer Stem Cell Agent Ipafricept (OMP-54F28), a Decoy Receptor for Wnt Ligands, in Patients with Advanced Solid Tumors. Clin Cancer Res. 2017 Dec 15;23(24):7490-7497. DOI:10.1158/1078-0432.CCR-17-2157
[2] Fischer MM, et al. WNT antagonists exhibit unique combinatorial antitumor activity with taxanes by potentiating mitotic cell death. Sci Adv. 2017 Jun 21;3(6):e1700090. DOI:10.1126/sciadv.1700090
[3] Li Y, et al. Peptide RL-QN15 regulates epidermal stem cell function to accelerate wound healing via the FZD8/β-catenin axis[J]. Authorea Preprints, 2024. |
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