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Cat. No.: HY-185816

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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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Please store the product under the recommended conditions in the Certificate of Analysis.

TQB2102 Chemical Structure

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform EGFR :

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In Vitro

Anti-cancerDNA Damage Response

Anti-cancer

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].

Anti-cancer

TQB2102 (144 h) exhibits bystander killing activity against HER2-negative MDA-MB-468 cells when co-cultured with HER2-positive KPL-4 cells^[2].

Anti-cancer

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].

Anti-cancer

DNA Damage Response

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.

In Vivo

Anti-cancerOthers

Anti-cancer

TQB2102 (0.5-5.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in the NCI-N87 gastric cancer xenograft model^[2].

Anti-cancer

TQB2102 (0.5-5.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in BT-474 breast cancer xenografts^[2].

Anti-cancer

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].

Others

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.

Animal Model:

nude mice (female)^[2]
Dosage:

0.5 mg/kg; 1.5 mg/kg; 5.0 mg/kg
Administration:

i.v.; single dose
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.

Animal Model:

nude mice (female)^[2]
Dosage:

0.5 mg/kg; 1.5 mg/kg; 5.0 mg/kg
Administration:

i.v.; single dose
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.

Animal Model:

nude mice (female)^[2]
Dosage:

1.0 mg/kg; 3.0 mg/kg; 10.0 mg/kg
Administration:

i.v.; single dose
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.

Related Protocols :

Chemical Information

SMILES

[TQB2102]
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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TQB2102

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