Cofetuzumab pelidotin
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.18%
- CAS No.: 1869937-48-3
- Molecular Weight:151784 (average)
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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 T1/2 of less than 3 days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6- to 10-week-old NOD scid mice with NSCLC, OVCA and TNBC cells[1]
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Dosage:3 mg/kg
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Administration:Intraperitoneal injection twice a week for four cycles
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Result:Induced striking in vivo anti-tumor effects on a subset of patient–derived xenografts (PDXs) derived from NSCLC, OVCA and TNBC.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
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Human IgG1 kappa
Chemical Information
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CAS No. 1869937-48-3
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Appearance Liquid
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Molecular Weight 151784 (average)
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Color Colorless to light yellow
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SMILES
[Cofetuzumab pelidotin]
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Synonyms
PF-06647020; ABBV-647; h6M24-vc0101
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Shipping
Shipping with dry ice.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (260 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)