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Background: PTK7 (Protein Tyrosine Kinase 7) is a pseudokinase of the receptor tyrosine kinase (RTK) family of Wnt receptors and shares a common ligand (Wnt5a) with fellow pseudokinases ROR1 (receptor tyrosine kinase-like orphan receptor 1) and ROR2. Despite the lack of a functional kinase domain PTK7 still contributes to downstream signaling of Wnt5a through its interaction with LRP6 (low-density lipoprotein receptor-related protein 6) and FZD (frizzled) receptors. PTK7 expression contributes to oncogenic potential in a variety of solid tumors including ovarian, colorectal and breast cancers and neuroblastoma. The cell surface expression and oncogenic function of PTK7 in a variety of tumor types makes it a compelling target for both CAR (chimeric antigen receptor)-T cell and antibody based therapeutic development. The use of cofetuzumab pelidotin, an ADC (antibody-drug conjugate) based on auristatin and targeting PTK7, showed promise in the treatment of ovarian cancer, NSCLC (non-small cell lung cancer) and TNBC (triple-negative breast cancer), showing the potential of targeting PTK7 in oncology.
CAS Number: 1869937-48-3
Description: Cofetuzumab pelidotin (PF-06647020) is a PTK7-targeting ADC comprising a humanized anti-PTK7 mAb (hu6M024, IgG1) joined to an auristatin microtubule inhibitor payload, auristatin-0101 (Aur0101), by a cleavable valine-citrulline (vc)-based linker. Cofetuzumab pelidotin has a DAR of 4. Cofetuzumab pelidotin binds to cell-surface PTK7 with an EC50 of 1153 pM by flow cytometry. Cofetuzumab pelidotin has the potential for solid tumors research1,2,3.
Format: Aqueous buffer solution.
Purity: ≥90%
Storage Stability: Store at -80°C, protect from light.
Target: PTK7
Uniprot: Q13308
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Marc Damelin, et al., 2017 Sci Transl Med. 9(372):eaag2611. 2. Chao Kong, et al., 2023 Mol Cancer Ther. 22(10):1128-1143. 3. Masaru Katoh, 2017 Transl Med. 5(23):462.
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