Trastuzumab vedotin
Based on 3 publication(s) in Google Scholar
Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma.
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- Reinheit: 98.05%
- Molecular Weight:150626 (average)
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Speicherung:
-80°C, protect from light
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Trastuzumab vedotin
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Biologische Aktivität
Trastuzumab vedotin (0.0128-1000 ng/mL; 60 min; RT) selectively binds to HER2 proteins of humans and monkeys, while no binding to HER2 proteins of rats or mice is observed[1].
Trastuzumab vedotin (4 μg/mL; 30 min, 37 °C) is efficiently internalized by human breast cancer SKBR3 cells at 37 °C, with an internalization rate comparable to that of its unconjugated antibody component MAB802[1].
Trastuzumab vedotin (4 μg; 4 h) exhibits no significant CDC activity against SKBR3 human breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKBR3 (high HER2), BT-474 (high HER2), MDA-MB-453 (medium HER2) human breast cancer cell lines; NCI-N87 (high HER2) human gastric cancer cell line
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Concentration:0.02 ng/mL-200 μg/mL
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Incubation Time:96 ± 2 h
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Result:Displayed potent sub-nanomolar cytotoxicity across all tested cell lines, with IC50 values of 0.012 nM (SKBR3), 0.035 nM (BT-474), 0.398 nM (MDA-MB-453), and 0.151 nM (NCI-N87). Its cytotoxicity was stronger than that of Kadcyla® in all high HER2-expressing cell lines tested.
Trastuzumab vedotin (MRG002) (1-10 mg/kg; i.v.; dosing schedule matching qw ×3 or equivalent) exhibits potent antitumor activity in trastuzumab-resistant HER2-expressing breast cancer PDX models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c naked mice (immunodeficient)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.v.; once weekly; 3 doses
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Result:Significantly inhibited tumor growth at all tested doses.\nMaintained suppressed tumor volume relative to vehicle controls at 0.3 mg/kg.\nFurther reduced tumor growth at 1 mg/kg, with a relative tumor growth (T/C) value of 45%.\nMaintained tumor volume near baseline levels at 3 mg/kg, with a relative tumor growth (T/C) value of 0%, corresponding to strong antitumor activity (++++).
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Animal Model:BALB/c naked mice (immunodeficient)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.v.; once weekly; 3 doses
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Result:Significantly inhibited tumor growth relative to vehicle controls at all tested doses.\nReduced tumor volume compared to vehicle at 0.3 mg/kg.\nStrongly suppressed tumor growth at 1 mg/kg.\nMaintained tumor volume near baseline levels at 3 mg/kg.
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Animal Model:BALB/c naked mice (immunodeficient)[1]
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Dosage:1 mg/kg (BC#046); 3 mg/kg (BC#046, BC#197, BC#239); 10 mg/kg (BC#197, BC#239)
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Administration:i.v.; dosing schedule matching qw ×3 or equivalent
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Result:In BC#046 model, reached a relative tumor growth (T/C) of 45% at 1 mg/kg (++ activity) and 0% at 3 mg/kg (++++ activity).\nIn BC#197 model, reached a relative tumor growth (T/C) of 14% at 3 mg/kg and 2% at 10 mg/kg (++++ activity at both doses).\nIn BC#239 model, reached a relative tumor growth (T/C) of 10% at 3 mg/kg and 3% at 10 mg/kg (++++ activity at both doses).\nShowed stronger antitumor activity than the reference drug at equivalent doses.
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Animal Model:Hu-HSC-NPG humanized mice (NPG mice transplanted with human CD34+ hematopoietic stem cells)[1]
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Dosage:3 mg/kg
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Administration:i.v.; once every 3 weeks; 2 doses
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Result:Significantly inhibited tumor growth relative to vehicle controls as a single agent.\nEnhanced antitumor activity when combined with an anti-PD-1 antibody (HX008), with a statistically significant difference (p < 0.05) observed on Day 21 compared to the target reagent alone.
Chemical Information
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Appearance Liquid
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Molecular Weight 150626 (average)
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Color Colorless to light yellow
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SMILES
[Trastuzumab MMAE]
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Synonyms
MRG002; Trastuzumab MMAE
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Versand
Shipping with dry ice.
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Speicherung
-80°C, protect from light
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Supramolecular coiled-coil peptide platform for site-specific antibody drug conjugate engineering. [Abstract]2026 Mar 2. PMID: 41771920 -
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Reinheit & Dokumentation
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Data Sheet (274 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)
Verweise
[1]. Li H, et al. Preclinical evaluation of MRG002, a novel HER2-targeting antibody-drug conjugate with potent antitumor activity against HER2-positive solid tumors. Antib Ther. 2021;4(3):175-184. Published 2021 Aug 28. [Content Brief]
[2]. Qu W, et al. A single-arm, multicenter, phase 2 clinical study of recombinant humanized anti-HER2 monoclonal antibody-MMAE conjugate (MRG002) in HER2-positive unresectable locally advanced or metastatic urothelial carcinoma. Eur J Cancer. 2024;205:114096. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Trastuzumab vedotin Related Classifications
HY-164992 Related Classifications
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- Trastuzumab vedotin
- MRG002
- Trastuzumab MMAE
- MRG 002
- MRG-002
- Antibody-Drug Conjugates (ADCs)
- EGFR
- Microtubule/Tubulin
- xenograft models
- anti-PD-1 antibody
- gastric cancer
- BT-474 human breast cancer cells
- SKBR3 human breast cancer cells
- breast cancer
- HER2
- lysosomes
- PDX models
- urothelial carcinoma
- Inhibitor
- inhibitor
- inhibit