2. Antibody-drug Conjugate/ADC Related Protein Tyrosine Kinase/RTK JAK/STAT Signaling Cell Cycle/DNA Damage Cytoskeleton
  3. Antibody-Drug Conjugates (ADCs) EGFR Microtubule/Tubulin
  4. Trastuzumab vedotin

Trastuzumab vedotin  (Synonyms: MRG002; Trastuzumab MMAE)

Cat. No.: HY-164992 Purity: 96.82%
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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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Trastuzumab vedotin

Trastuzumab vedotin Chemical Structure

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Trastuzumab vedotin Related Antibodies

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2 Publications Citing Use of MCE Trastuzumab vedotin

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Description

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[1][2].

In Vitro

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.

Trastuzumab vedotin Related Antibodies

Cell Cytotoxicity Assay[1]

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
Concentration: 0.02 ng/mL-200 μg/mL
Incubation Time: 96 ± 2 h
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.
In Vivo

Trastuzumab vedotin (MRG002) (0.3-3 mg/kg; i.v.; once weekly; 3 doses) exhibits potent, dose-dependent antitumor activity in BT-474 breast cancer xenografts, with complete tumor growth suppression observed at 3 mg/kg[1].
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.

Animal Model: BALB/c naked mice (immunodeficient)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: i.v.; once weekly; 3 doses
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 (++++).
Animal Model: BALB/c naked mice (immunodeficient)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: i.v.; once weekly; 3 doses
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.
Animal Model: BALB/c naked mice (immunodeficient)[1]
Dosage: 1 mg/kg (BC#046); 3 mg/kg (BC#046, BC#197, BC#239); 10 mg/kg (BC#197, BC#239)
Administration: i.v.; dosing schedule matching qw ×3 or equivalent
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.
Animal Model: Hu-HSC-NPG humanized mice (NPG mice transplanted with human CD34+ hematopoietic stem cells)[1]
Dosage: 3 mg/kg
Administration: i.v.; once every 3 weeks; 2 doses
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.
Molecular Weight

150626 (average)

Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Trastuzumab MMAE]
Shipping

Shipping with dry ice.
Storage

-80°C, protect from light
Purity & Documentation

Purity: 96.82%

SDS (251 KB)

COA (231 KB) SEC-HPLC (125 KB)

Handling Instructions (2659 KB)
References
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Trastuzumab vedotin Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trastuzumab vedotinMRG002 Trastuzumab MMAEMRG 002MRG-002Antibody-Drug Conjugates (ADCs)EGFRMicrotubule/TubulinAntibody-Drug ConjugatesEpidermal growth factor receptorErbB-1HER1xenograft modelsanti-PD-1 antibodygastric cancerBT-474 human breast cancer cellsSKBR3 human breast cancer cellsbreast cancerHER2lysosomesPDX modelsurothelial carcinomaInhibitorinhibitorinhibit

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