Linker Information
General Information of This Linker
Linker ID |
LIN0NNRAU
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Linker Name |
Azadibenzocylooctyne-amine derivative 6d
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Linker Type |
Bioorthogonal reaction linker
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Antibody-Linker Relation |
Cleavable
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
HER2-gsADC-5 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 26.50% (Day 51) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
HER2-gsADC-49 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
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Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
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Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 66.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
References
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