TQB2102
TQB2102 is a bispecific epitope antibody-drug conjugate targeting HER2, composed of the antibody Rolditamig (HY-P992130) and the toxin molecule Deruxtecan-d2 (HY-13631ES3). TQB2102 binds to the ECD2 and ECD4 domains of HER2, promotes its own internalization by HER2-expressing cells, and delivers deuterated DXd payload to inhibit topoisomerase I. TQB2102 induces antibody-dependent cellular cytotoxicity, DNA damage, bystander killing activity, and inhibits cancer cell proliferation. TQB2102 can be used in research related to various cancers including metastatic breast cancer, colorectal cancer, and gastric/gastroesophageal junction adenocarcinoma.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
体外実験
TQB2102 (6 h) induces antibody-dependent cell-mediated cytotoxicity (ADCC) in human gastric cancer cell line NCI-N87, with an EC50 of 2.33 ng/mL[2].
TQB2102 (144 h) exhibits bystander killing activity against HER2-negative MDA-MB-468 cells when co-cultured with HER2-positive KPL-4 cells[2].
TQB2102 (44 h) potently inhibits the proliferation of NCI-N87 cells with high HER2 expression, Trastuzumab emtansine (HY-P9921)-resistant NCI-N87/16-8 cells, and BT-474 cells with moderate HER2 expression, with IC50 values of 66.7 ng/mL, 74.3 ng/mL, and 116.2 ng/mL, respectively, but exerts no inhibitory effect on JIMT-1 cells with low HER2 expression[2].
TQB2102 induces DNA damage, an effect detected by increased phosphorylation levels of γ-H2AX, and this phenomenon occurs in human cancer cell lines NCI-N87 and JIMT-1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
TQB2102 (0.5-5.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in BT-474 breast cancer xenografts[2].
TQB2102 (1.0-10.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in the COLO 205 colorectal cancer xenograft model[2].
TQB2102 (3.0-30.0 mg/kg; intravenous injection; once every 2 weeks; 3 or 7 doses) is well tolerated in cynomolgus monkeys. No significant pulmonary toxicity or organ system damage is observed at the highest dose of 30.0 mg/kg administered once every 2 weeks[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nude mice (female)[2]
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Dosage:0.5 mg/kg; 1.5 mg/kg; 5.0 mg/kg
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Administration:i.v.; single dose
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Result:Exhibited dose-dependent tumor growth inhibition, with tumor inhibition rates (TIRs) of 44.0% at 0.5 mg/kg, 76.0% at 1.5 mg/kg, and 102.0% at 5.0 mg/kg.
Showed good tolerability in all tumor-bearing mice, with no significant weight loss reported.
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Animal Model:nude mice (female)[2]
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Dosage:0.5 mg/kg; 1.5 mg/kg; 5.0 mg/kg
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Administration:i.v.; single dose
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Result:Exhibited dose-dependent tumor growth inhibition, with TIRs of 13.0% at 0.5 mg/kg, 16.0% at 1.5 mg/kg, and 92.0% at 5.0 mg/kg.
Caused a maximum weight loss of 3.7% on day 9 at the 5.0 mg/kg dose, with no other significant toxicity reported.
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Animal Model:nude mice (female)[2]
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Dosage:1.0 mg/kg; 3.0 mg/kg; 10.0 mg/kg
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Administration:i.v.; single dose
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Result:Exhibited dose-dependent tumor growth inhibition, with TIRs of 12.7% at 1.0 mg/kg, 41.2% at 3.0 mg/kg, and 81.0% at 10.0 mg/kg.
Showed good tolerability in all tumor-bearing mice, with no significant weight loss reported.
- Mammalian live/dead viability and cytotoxicity staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Cell Cytotoxicity Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
- Genotoxicity/Mutagenicity Study
化学情報
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SMILES
[TQB2102]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Zhang, et al. Antibody drug conjugate. WO2022033578.
[2]. Ruan DY, et al. Preclinical characterization and phase I results of TQB2102, a first-in-class HER2 biparatopic antibody-drug conjugate, in patients with advanced solid tumors. Annals of oncology : official journal of the European Society for Medical Oncology. 2026 May 15. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TQB2102 関連分類
HY-185816 関連分類
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