Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0CDBRB
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| ADC Name |
TZ-dSA3-12
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| Synonyms |
TZ-dSA3-12
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| Organization |
Qingdao University.; Capital Medical University.; Academy of Military Medical Sciences.; Chinese Academy of Medical Sciences & Peking Union Medical College.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
2.1
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| Structure |
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| Antibody Name |
Trastuzumab
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
diABZI STING agonist 3
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Payload Info | ||||
| Therapeutic Target |
Stimulator of interferon genes protein (STING)
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Target Info | ||||
| Linker Name |
Undisclosed
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| Conjugate Type |
Site specific conjugation at HC-A140C.
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ADC-specific functional property(2027 Update)
Payload Release Efficiency
| Incubation Time | 6h | Release | 52.96% | Reference |
[1]
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| Description |
In vitro studies revealed that in the presence of CTSB enzymes, TZ-dSA3-12 can release 52.96% of the drug within 6 hours and achieve a complete release in 24 h
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| Incubation Time | 24h | Release | 100% | Reference |
[1]
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| Description |
In vitro studies revealed that in the presence of CTSB enzymes, TZ-dSA3-12 can release 52.96% of the drug within 6 hours and achieve a complete release in 24 h
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Circulating Stability
| Incubation Time | 14day | Release | <1.5% | Reference |
[1]
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| Incubation Medium | Human serum | ||||
| Description |
Furthermore, TZ-dSA3-12 demonstrated a release of less than 1.5% of the total dSA3 payload over a 14-day period in human plasma (Figure 3e), suggesting favorable plasma stability.
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Tumor Growth lnhibition value (TGl) |
87.71
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%
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Undisclosed | Undisclosed |
| Tumor Growth lnhibition value (TGl) |
89.75
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%
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Undisclosed | Undisclosed |
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
87.71%
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| Method Description |
Compared to the PBS control group, the TZ-dSA3-12 (1 and 3mg kg-1) treatment group displayed significant and sustained suppression of tumor growth with an inhibition rate of 87.71% and 89.75%
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| In Vivo Model | N87 tumor-bearing BALB/c nude mice | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
89.75%
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| Method Description |
Compared to the PBS control group, the TZ-dSA3-12 (1 and 3mg kg-1) treatment group displayed significant and sustained suppression of tumor growth with an inhibition rate of 87.71% and 89.75%
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| In Vivo Model | N87 tumor-bearing BALB/c nude mice | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.08 nM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.11- 0.28 nM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.13 nM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
References