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3G1-Fc is a bivalent recombinant fusion protein antibody in the scFv-Fc format that specifically targets the KIT receptor (CD117), a type III receptor tyrosine kinase. 3G1-Fc binds to the D5 membrane proximal region of KIT, acts as an antagonist, and does not stimulate KIT phosphorylation or downstream signaling on its own. Instead, it inhibits stem cell factor (SCF)-induced KIT signaling, leading to decreased cell viability and growth of KIT-dependent leukemic cell lines. 3G1-Fc also induces internalization and down-regulation of KIT from the cell surface, an effect that is enhanced in combination with tyrosine kinase inhibitors such as imatinib. The antibody thereby reduces oncogenic KIT signaling, which is implicated in several leukemias and mast cell disorders.
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