Ginisortamab (UCB6114) is a fully human IgG4P anti Gremlin-1 monoclonal antibody, with mean IC₅₀ values of 8.2 nM and 9 nM against human and mouse gremlin-1, respectivly. Ginisortamab inhibits gremlin-1 antagonism of BMP signaling pathways. Ginisortamab has the potential for the research of gastrointestinal (GI) tumors^[1][2][3].

Human IgG4 kappa

Human IgG4 (S228P) kappa, Isotype Control

Human

GREM1/Gremlin

Ginisortamab (0.1-1000 nM) inhibits both human and mouse gremlin-1 in a concentration-dependent manner, with mean IC₅₀ values of 8.2 nM and 9 nM, respectively^[2].
The geometric mean affinities (equilibrium dissociation constant [K_D]) of Ginisortamab for human and mouse gremlin-1 are 87 pM and 61 pM, respectively^[2].
Ginisortamab (150 nM, 30-120 min) inhibits gremlin-1 antagonism of BMP signaling pathways in human CRC cell and fibroblasts lines^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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  Human IgG4 kappa

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  Immobilized Human Gremlin/GREM1 Protein, His Tag can bind Ginisortamab. The EC₅₀ for this effect is 10.22 ng/mL.
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  Flow cytometric analysis of 1X10⁶ SH-SY5Y cells labeling GREM1 with Ginisortamab (HY-P99643, red). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then stained with the primary antibody at 1/200 for an hour at 4℃. AF488-conjugated Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG4 kappa Isotype Control (HY-P99003, blue) was used as the isotype control.

• [1]. Debashis Sarker, et al. A multi-modular phase I/II study of UCB6114, a first-in-class, fully human IgG4P anti-Gremlin-1 monoclonal antibody, as monotherapy and in combination with mFOLFOX6 or trifluridine/tipiracil, for patients with advanced gastrointestinal (GI) tumors. Meeting Abstract, 2022 ASCO Gastrointestinal Cancers Symposium.

  [2]. Davies GCG, et al. Discovery of ginisortamab, a potent and novel anti-gremlin-1 antibody in clinical development for the treatment of cancer. MAbs. 2023 Jan-Dec;15(1):2289681.  [Content Brief]

  [3]. Debashis Sarker, et al. Abstract CT094: Phase I dose-escalation study evaluating the safety and tolerability of ginisortamab (UCB6114), a first-in-class anti-gremlin-1 monoclonal antibody (mAb), as monotherapy in advanced solid tumors. Cancer Res (2023) 83 (8_Supplement): CT094 .