Patritumab deruxtecan
Based on 1 publication(s) in Google Scholar
Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) targeting HER3, consisting of the anti-HER3 IgG1 antibody Patritumab (HY-P99275), a cleavable tetrapeptide linker, and the membrane-permeable topoisomerase I (Topoisomerase Ⅰ) inhibitor DXd (HY-13631D). After binding to membrane-localized HER3, Patritumab deruxtecan is internalized into lysosomes, where the linker is cleaved to release DXd. DXd enters the nucleus to induce DNA damage and cell death, and exerts a bystander effect via transmembrane diffusion. Patritumab deruxtecan reduces the viability of HER3-positive cells and induces features of immunogenic cell death including CALR membrane exposure, ATP and HMGB1 release, and can be used in studies related to HER3-positive breast cancer and non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 99.08%
- CAS No.: 2227102-46-5
- Molecular Weight:155238 (average)
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Storage:
-80°C, protect from light
Publications Citing Use of MedChemExpress (MCE) Patritumab deruxtecan
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Biological Activity
Description
IC50 & Target
[1]|
HER3 |
In Vitro
Patritumab deruxtecan (HER3-DXd) (0.04-10 µg/mL; 5 days) decreases viability and induces calreticulin relocation in HER3-overexpressing U2OS-CALR-GFP cells, but not in parental HER3-negative U2OS-CALR-GFP cells[3].
Patritumab deruxtecan (0.16 µg/mL; 5 days) induces hallmarks of immunogenic cell death, including calreticulin surface exposure, extracellular ATP release, and HMGB1 release, in HER3-overexpressing U2OS cells, but not in parental HER3-negative U2OS cells[3].
Patritumab deruxtecan (0.16 µg/mL; 5 days) induces bystander antitumor effects, reducing viability of HER3-negative U2OS cells when cocultured with HER3-overexpressing U2OS cells[3].
Patritumab deruxtecan (0.16 µg/mL; 5 days) releases its cytotoxic payload DXd into cell culture supernatants when applied to HER3-overexpressing U2OS cells, either alone or in coculture with HER3-negative U2OS cells[3].
Patritumab deruxtecan (0.1-100 nM; 1 h) binds specifically and with comparable affinity to MDA-MB-231 cells expressing HER3 wild type or clinically reported HER3G12C mutations, regardless of HER2 overexpression, with no binding to HER3-negative MDA-MB-231 cells[4].
Patritumab deruxtecan (10 nM; 6 days) significantly inhibits the growth of MDA-MB-231 cells expressing HER3 wild type or most clinically reported HER3 mutations, with activity observed regardless of HER2 overexpression, and no activity against HER3-negative MDA-MB-231 cells[4].
Patritumab deruxtecan (0.1-10 nM; up to 12 h) undergoes time- and concentration-dependent lysosomal trafficking in MDA-MB-231 cells expressing HER3 wild type or clinically reported HER3G12C mutations, at comparable levels regardless of HER2 overexpression, with minimal trafficking in HER3-negative MDA-MB-231 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human osteosarcoma U2OS cells (HER3-negative, differentially tagged), HER3-overexpressing U2OS cells
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Concentration:0.16 µg/mL
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Incubation Time:5 days
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Result:Significantly reduced the viability of both HER3-overexpressing U2OS cells and HER3-negative bystander U2OS cells in the coculture.
Did not affect viability of HER3-negative U2OS cells in monoculture.
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Cell Line:MDA-MB-231 human triple-negative breast cancer cells transduced with HER3 wild type (HER3WT), 11 HER3 mutations, or HER3 empty vector (HER3EV), in the presence or absence of HER2 overexpression
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Concentration:10 nM
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Incubation Time:6 days
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Result:Showed significant growth-inhibitory activity against HER3WT cells.
Exhibited growth-inhibitory activity against most HER3-mutant cells.
Showed no inhibitory activity against HER3EV cells.
Had minimal impact of HER2 overexpression on growth inhibition, though substantial inhibition was not observed in cells expressing HER3 mutations V104M, G325R, and S846I without HER2 overexpression.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2227102-46-5
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Appearance Liquid
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Molecular Weight 155238 (average)
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Color Colorless to light yellow
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SMILES
[Patritumab deruxtecan]
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Synonyms
HER3-DXd; U3-1402
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Shipping
Shipping with dry ice.
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Storage
-80°C, protect from light
Publications (1)
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Journal Impact Factor
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Most Recent
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)