Disitamab vedotin是一种靶向HER2蛋白的抗体药物偶联物，由hertuzumab通过可裂解连接子与monomethyl auristatin E (MMAE)偶联而成。
Cas No.:2136633-23-1
Sample solution is provided at 25 µL, 10mM.
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Disitamab vedotin is an antibody-drug conjugate (ADC) targeting HER2 protein that is comprised of hertuzumab coupling monomethyl auristatin E (MMAE) via a cleavable linker [1]. Disitamab vedotin can kill tumor cells by targeting HER2-protein on the surface of tumor cells, as well as releasing small molecules in lysosomes after endocytosis[2]. Disitamab vedotin has been widely used to inhibit the growth of various drug-resistant cancer cells and tumors in xenograft mouse models[3].
In vitro, Disitamab vedotin treatment for 48 hours significantly inhibited the growth of HT1376 cells, SW780 cells and RT4 cells was, with IC50 values of 158.3μg/ml, 155.7μg/ml and 132.2μg/ml, respectively[4]. Treatment with 50μg/ml Disitamab vedotin for 48 hours impeded the transition from G1 phase to S phase in A549 cells, increased the apoptosis rate and decreased the expression of FOXA1 protein[5]. Treatment with 100μg/ml Disitamab vedotin for 48 hours activated the cGAS-STING pathway in HCT116 cells, inducing cell cycle arrest[6].
In vivo, Disitamab vedotin treatment via weekly intravenous administration of 2.5mg/kg for 3 weeks significantly reduced the tumor volume in the CRC054 xenograft mouse model, without showing any obvious organ toxicity[7]. A single intravenous injection of 5mg/kg of Disitamab vedotin can inhibit tumor growth in the L-JIMT-1 lung metastasis mouse model and reduce vascular volume[8].
References:
[1] Shi F, Liu Y, Zhou X, et al. Disitamab vedotin: a novel antibody-drug conjugates for cancer therapy[J]. Drug Delivery, 2022, 29(1): 1335-1344.
[2] Jiang J, Li S, Shan X, et al. Preclinical safety profile of disitamab vedotin: a novel anti-HER2 antibody conjugated with MMAE[J]. Toxicology letters, 2020, 324: 30-37.
[3] Pourjamal N, Le Joncour V, Vereb G, et al. Disitamab vedotin in preclinical models of HER2-positive breast and gastric cancers resistant to trastuzumab emtansine and trastuzumab deruxtecan[J]. Translational oncology, 2025, 53: 102284.
[4] Li J, Shan K, Huang W, et al. The combination treatment of RC48 and STAT3 inhibitor acts as a promising therapeutic strategy for basal bladder cancer[J]. Frontiers in immunology, 2025, 15: 1432586.
[5] Zhao M, Zhang N, Wang Y, et al. FOXA1, induced by RC48, regulates HER2 transcription to enhance the tumorigenic capacity of lung cancer through PI3K/AKT pathway[J]. Journal of Cancer, 2024, 15(18): 5863.
[6] Wu X, Xu L, Li X, et al. A HER2-targeting antibody-MMAE conjugate RC48 sensitizes immunotherapy in HER2-positive colon cancer by triggering the cGAS-STING pathway[J]. Cell Death & Disease, 2023, 14(8): 550.
[7] Liu H, Zhou D, Liu D, et al. Synergistic antitumor activity between HER2 antibody-drug conjugate and chemotherapy for treating advanced colorectal cancer[J]. Cell Death & Disease, 2024, 15(3): 187.
[8] Pourjamal N, Yazdi N, Halme A, et al. Comparison of trastuzumab emtansine, trastuzumab deruxtecan, and disitamab vedotin in a multiresistant HER2-positive breast cancer lung metastasis model[J]. Clinical & Experimental Metastasis, 2024, 41(2): 91-102.
Disitamab vedotin是一种靶向HER2蛋白的抗体药物偶联物，由hertuzumab通过可裂解连接子与monomethyl auristatin E (MMAE)偶联而成[1]。Disitamab vedotin既可通过靶向肿瘤细胞表面的HER2蛋白杀伤肿瘤细胞，也可在内吞后于溶酶体中释放小分子发挥作用[2]。Disitamab vedotin已被广泛用于抑制异种移植小鼠模型中多种耐药癌细胞和肿瘤的生长[3]。
在体外，Disitamab vedotin处理48小时显著抑制了HT1376细胞、SW780细胞和RT4细胞的生长，IC50值分别为158.3μg/ml、155.7μg/ml和132.2μg/ml [4]。用50μg/ml的Disitamab vedotin处理A549细胞48小时，阻碍了细胞从G1期向S期的转变，增加了凋亡率并降低了FOXA1蛋白的表达[5]。用100μg/ml的Disitamab vedotin处理HCT116细胞48小时，激活了cGAS-STING通路，诱导了细胞周期阻滞[6]。
在体内，每周静脉注射2.5mg/kg剂量的Disitamab vedotin，连续3周，显著减少了CRC054异种移植小鼠模型中的肿瘤体积，且未表现出明显的器官毒性[7]。单次静脉注射5mg/kg剂量的Disitamab vedotin，可抑制L-JIMT-1肺转移小鼠模型中的肿瘤生长并减少血管体积[8]。
| Cell experiment [1]: | |
Cell lines | HT1376 cells |
Preparation Method | HT1376 cells were grown in DMEM medium supplemented with 10% fetal bovine serum, 100U/ml penicillin, and 0.1mg/ml streptomycin in 5% CO2 at 37°C. 5×103 HT1376 cells/ml were seeded into 96-well microplates for 24h. The wells were replenished with fresh complete medium containing different concentrations of Disitamab vedotin (0, 1, 10, 50, 100, and 200µg/ml) for 48h. Then, the cell viability was detected. |
Reaction Conditions | 0, 1, 10, 50, 100, and 200µg/ml; 48h |
Applications | Disitamab vedotin treatment significantly decreased the cell viability of HT1376 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | BALB/c nude mice (6 weeks old) were kept in temperature-controlled (21°C-25°C) and humidity-maintained (40%-70%) rooms with a 12-h light/dark cycle. Water and food were provided freely. 5×106 HCT116 cells suspended in 100μl PBS were injected subcutaneously into the right flank of mice. When the tumor volume reached 100 to 150mm3, the mice were randomized into 2 groups and injected intravenously with Disitamab vedotin (5mg/kg) for 3 weeks. Tumor sizes and body weight were recorded twice a week, and tumor volumes were determined according to the formula: tumor volume (mm3)=length×(width)2×0.5. |
Dosage form | 5mg/kg; once a week for 3 weeks; i.v. |
Applications | Disitamab vedotin treatment significantly inhibited tumor growth in the HCT116 mouse xenograft model. |
References: | |
| Cas No. | 2136633-23-1 | SDF | Download SDF |
| 别名 | DISITAMABVEDOTIN(纬迪西妥单抗),RC48 | ||
| 分子式 | 分子量 | 144.15 kDa(Approximately) | |
| 溶解度 | 储存条件 | Store at -20°C,protect from light | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 6.9 μL | 34.7 μL | 69.4 μL |
| 5 mM | 1.4 μL | 6.9 μL | 13.9 μL |
| 10 mM | 0.7 μL | 3.5 μL | 6.9 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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Purity: >97.00%
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