Disitamab vedotin
Based on 5 publication(s) in Google Scholar
Disitamab vedotin (RC48) is a HER2-targeted antibody-drug conjugate (ADC), formed by conjugation of the humanized anti-HER2 antibody Disitamab (HY-P99854) with drug-linker VcMMAE (HY-15575). VcMMAE consists of a cleavable MC-Val-Cit-PAB linker and the microtubule inhibitor MMAE (HY-15162). After binding to HER2 and undergoing endocytosis, Disitamab vedotin releases MMAE in lysosomes, which further inhibits microtubule assembly, arrests mitosis and induces apoptosis, while also exerting a bystander effect. Disitamab vedotin can be used in studies of HER2-positive breast cancer.
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- Reinheit: 99.06%
- CAS. Nr.: 2136633-23-1
- Molecular Weight:149000 (average)
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Biologische Aktivität
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HER2 |
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Cell Line
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Type | Value | Description | References |
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| E0771 | IC50 |
90 ng/mL
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Reduction of murine breast cancer E0771-hHER2 cell viability incubated for 96 hrs assessed via Cell Counting Kit-8 (CCK-8) metabolic activity assay.
Reduction of murine breast cancer E0771-hHER2 cell viability incubated for 96 hrs assessed via Cell Counting Kit-8 (CCK-8) metabolic activity assay.
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34657203 |
Disitamab vedotin (RC48) exerts a significant bystander killing effect in vitro against heterogeneous HER2-expressing cancer cell populations, enhancing its efficacy by targeting both HER2-positive and adjacent HER2-negative tumor cells[3].
Disitamab vedotin (0.0001-10 µg/mL; 48-96 h) potently inhibits E0771-hHER2 murine breast cancer cell viability with an IC50 of 90 ng/mL, with target-specific activity and no effect on hHER2-negative E0771-WT cells[2].
Disitamab vedotin (10.0 μg/mL) shows specific cross-reactivity to normal human tissues including bladder, skin, breast, pancreas, placenta, kidney, prostate, ureter, fallopian tube, and stomach[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:E0771-hHER2; E0771-WT
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Concentration:100, 500 ng/mL
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Incubation Time:48, 72 h
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Result:Preferentially reduced viability of E0771-hHER2 cells compared with E0771-WT cells.
Combination treatment with Disitamab vedotin (5 mg/kg; i.v.; Days 0, 7) and anti-PD-1 antibody (HY-P9902A) (10 mg/kg; i.v.; Days 0, 3, 7, 10) significantly inhibits the growth of E0771-hHER2 tumors and leads to tumor regression in the combination group within approximately 2-3 weeks[2].
Disitamab vedotin (10 mg/kg; single i.v. administration) increases T cell infiltration in tumor tissues of E0771-hHER2 tumor-bearing mice[2].
Combination therapy with disitamab vedotin and a PD-1/PD-L1 checkpoint inhibitor induces durable immune protection in mice with completely regressed E0771-hHER2 tumors; complete tumor rejection occurs upon rechallenge with E0771-hHER2 cells, and a weaker rejection effect is also observed upon rechallenge with E0771-WT cells[2].
Disitamab vedotin (3-12 mg/kg; intravenous injection; once every 2 weeks; for 12 consecutive weeks) induces dose-dependent, reversible hematological and lymphoid organ toxicity in healthy cynomolgus monkeys, with a maximum non-severe toxic dose of 6 mg/kg, and the positive rate of anti-drug antibodies decreases with increasing dose[5].
Disitamab vedotin (4-16 mg/kg; intravenous injection; single administration) produces no treatment-related effects on the central nervous system of healthy Sprague Dawley rats at doses up to 16 mg/kg[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human PD-1 transgenic C57BL/6 (5 to 6 weeks old; subcutaneous inoculation of 2 × 106 E0771-hHER2 cells; treatment initiated when average tumor volume reached 100-200 mm3)[2]
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Dosage:10 mg/kg
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Administration:i.v.; single dose on day 5 post-tumor inoculation
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Result:Reduced mean tumor volume to 244.82 mm³ on day 9 after administration.
Increased intratumoral T cell infiltration relative to vehicle and parental anti-hHER2 antibody groups.
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Animal Model:Human PD-1 transgenic C57BL/6 (5 to 6 weeks old; subcutaneous inoculation of 2 × 106 E0771-hHER2 cells; treatment initiated when average tumor volume reached 150-200 mm3)[2]
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Dosage:5 mg/kg (monotherapy); 5 mg/kg + 10 mg/kg (anti-PD-1/PD-L1 antibody, combination)
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Administration:i.v.;Disitamab vedotin on days 0 and 7; anti-PD-1 on days 0, 3, 7, and 10
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Result:Combination markedly inhibited tumor growth and resulted in tumor disappearance within approximately 2-3 weeks.
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Animal Model:Cynomolgus monkeys (3.5-5 years old)[5]
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Dosage:3 mg/kg; 6 mg/kg; 12 mg/kg
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Administration:i.v.; every 2 weeks; 12 weeks
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Result:Produced dose-dependent hematological changes; the highest non-severely toxic dose was 6 mg/kg.
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Animal Model:Sprague Dawley rats (6-9 weeks old, n=5/sex/group)[5]
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Dosage:4 mg/kg; 8 mg/kg; 16 mg/kg
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Administration:i.v.; single dose
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Result:Showed no administration-related abnormalities in home-cage, hand-held, or open-field observations, stimulus responses, rearing counts, defecation counts, forelimb grip strength, or body temperature, with all parameters statistically similar to the negative control group.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2136633-23-1
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Appearance Solid
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Molecular Weight 149000 (average)
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Color White to light yellow
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SMILES
[Disitamab vedotin]
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Synonyms
RC48
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Preparation Instructions
The product can be reconstituted/diluted with sterile PBS or saline.
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Versand
Shipping with dry ice.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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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 -
Cancer Lett
Drug-tolerant persisting polyploid giant cancer cells mediate resistance to HER2-targeting antibody-drug conjugates. [Abstract]2025 Oct 10:630:217900. PMID: 40614854
Disitamab vedotin purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2025 Oct 10:630:217900. [Abstract]
Disitamab vedotin (DV, 0.25 μg/mL) reduced the overall cell number of HER2-positive JIMT-1 breast cancer cells.
Disitamab vedotin purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2025 Oct 10:630:217900. [Abstract]
Unlike the parental cells, which were sensitive to XMT-1522 and Disitamab vedotin (DV, 0.0001, 0.0006, 0.003, 0.016, 0.08, 0.4, 1, 2, and 10 μg/mL; 5 days), both D1 and D2 daughter cells that emerged from the DTP-PGCC were resistant to these drugs. D1, daughter-1 cells (one prior ADC treatment); D2, daughter-2 cells (two prior ADC treatments). ∗∗, p < 0.01; ∗∗∗, p < 0.001.
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Mol Cancer Ther
Antibody-drug-conjugates prepared with Peptide Asparaginyl Ligases achieve strong in vitro and in vivo anti-tumor activity. [Abstract]2026 Mar 26. PMID: 41889275 -
Transl Oncol
Disitamab vedotin in preclinical models of HER2-positive breast and gastric cancers resistant to trastuzumab emtansine and trastuzumab deruxtecan. [Abstract]2025 Mar:53:102284. PMID: 39837059
Disitamab vedotin purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2025 Mar:53:102284. [Abstract]
Disitamab vedotin (DV, 50 μg/mL, 15 or 30 min) increased T-DM1 internalization into JIMT-1 breast cancer cells.
Disitamab vedotin purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2025 Mar:53:102284. [Abstract]
In JIMT-1 xenografts, the combination of Disitamab vedotin (DV, 0.5 mg/kg or 5 mg/kg, administered intravenously twice at 7-day intervals) plus T-DM1, as well as DV plus T-DXd, inhibited tumor growth more effectively than the corresponding single treatments.
Disitamab vedotin purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2025 Mar:53:102284. [Abstract]
In macroscopic JIMT-1 xenografts, tumors that relapsed after T-DM1 treatment and subsequently responded to Disitamab vedotin (DV, 0.5 mg/kg or 5 mg/kg, administered intravenously twice at 7-day intervals) but later progressed had lost HER2 expression. A: PBS; B: relapsed after T-DM1, progressed on T-DM1; C: relapsed after T-DM1, progressed on DV; D: relapsed after T-DM1, progressed on T-DXd.
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Clin Exp Metastasis
Comparison of trastuzumab emtansine, trastuzumab deruxtecan, and disitamab vedotin in a multiresistant HER2-positive breast cancer lung metastasis model. [Abstract]2024 Apr;41(2):91-102. PMID: 38367127
Reinheit & Dokumentation
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Data Sheet (282 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]. Deeks ED, et al. Disitamab Vedotin: First Approval. Drugs. 2021 Nov;81(16):1929-1935. [Content Brief]
[2]. Huang L, et al. A HER2 target antibody drug conjugate combined with anti-PD-(L)1 treatment eliminates hHER2+ tumors in hPD-1 transgenic mouse model and contributes immune memory formation. Breast cancer research and treatment. 2022 Jan;191(1):51-61. [Content Brief]
[5]. Jiang J, et al. Preclinical safety profile of Disitamab vedotin: a novel anti-HER2 antibody conjugated with MMAE. Toxicology Letters. 2019. [Content Brief]
Calculators
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