Cofetuzumab pelidotin  (Synonyms: PF-06647020; ABBV-647; h6M24-vc0101)

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; HY-12522), 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 research^[1][2][3].

Cofetuzumab pelidotin (PF-06647020) shows in vitro cytotoxic effects on PTK7 expressing cancer cell lines H446, H661 and OVCAR3 with EC₅₀ values of 7.6, 27.5 and 105 ng/mL, respectively^[1].
Cofetuzumab pelidotin (PF-06647020) (for 6 days) shows high potency and PTK7-specific cytotoxicity in a panel of cancer cell lines (A549, MDA-MB-468, KYSE-150, SKOV-3, PC9, NCI-H1975 cells) with IC₅₀s of 0-1100 nM^[2].
Cofetuzumab pelidotin is less stable with a much shorter T_1/2 of less than 3 days^[2].

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

Cofetuzumab pelidotin (PF-06647020; 3 mg/kg; Intraperitoneal injection twice a week for four cycles) induces striking in vivo anti-tumor effects on a subset of PDXs derived from NSCLC, OVCA and TNBC^[1].

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

151784 (average)

1869937-48-3

Liquid

Colorless to light yellow

[Cofetuzumab pelidotin]

Shipping with dry ice.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  Human IgG1 kappa

• [1]. Marc Damelin, et al. A PTK7-targeted antibody-drug conjugate reduces tumor-initiating cells and induces sustained tumor regressions. Sci Transl Med. 2017 Jan 11;9(372):eaag2611.  [Content Brief]

  [2]. Chao Kong, et al. MTX-13, a Novel PTK7-Directed Antibody-Drug Conjugate with Widened Therapeutic Index Shows Sustained Tumor Regressions for a Broader Spectrum of PTK7-Positive Tumors. Mol Cancer Ther. 2023 Oct 2;22(10):1128-1143.  [Content Brief]

  [3]. Masaru Katoh. Antibody-drug conjugate targeting protein tyrosine kinase 7, a receptor tyrosine kinase-like molecule involved in WNT and vascular endothelial growth factor signaling: effects on cancer stem cells, tumor microenvironment and whole-body homeostasis. nn Transl Med. 2017 Dec;5(23):462.  [Content Brief]