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Research Grade Ipafricept (DHK29201)

Product NameResearch Grade Ipafricept (DHK29201)
CAS1391727-24-4
MF
MW0
EINECS
MOL FileMol File

Chemical Properties

form	Liquid
color	Colorless to light yellow

Usage And Synthesis

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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