Linker Information
General Information of This Linker
| Linker ID |
LIN0LJIKM
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| Linker Name |
N-hydroxysuccinimide based linker
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| Linker Type |
Flexible reactive (amino) linker
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| Antibody-Linker Relation |
Uncleavable
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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
Cet-TPL [Investigative]
Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 72.17% (Day 13) | Positive EGFR expression (EGFR +++/++) | ||
| Method Description |
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
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| In Vivo Model | Lung adenocarcinoma PDX model (PDX: PDX1) | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 91.89% (Day 15) | Positive EGFR expression (EGFR +++/++) | ||
| Method Description |
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
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| In Vivo Model | Lung adenocarcinoma PDX model (PDX: PDX1) | ||||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 12.39% (Day 15) | Negative EGFR expression (EGFR -) | ||
| Method Description |
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
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| In Vivo Model | H520 CDX model | ||||
| In Vitro Model | Lung squamous cell carcinoma | NCI-H520 cells | CVCL_1566 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 64.00% (Day 18) | Positive EGFR expression (EGFR +++/++) | ||
| Method Description |
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
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| In Vivo Model | A549 CDX model | ||||
| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 93.80% (Day 24) | Positive EGFR expression (EGFR +++/++) | ||
| Method Description |
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
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| In Vivo Model | SCC6 CDX model | ||||
| In Vitro Model | Squamous cell carcinoma | UM-SCC-6 cells | CVCL_7773 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.25 ug/mL - 12.5 ug/mL
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Positive EGFR expression (EGFR +++/++) | ||
| Method Description |
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
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| In Vitro Model | Squamous cell carcinoma | UM-SCC-6 cells | CVCL_7773 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
12.50 ug/mL
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Positive EGFR expression (EGFR +++/++) | ||
| Method Description |
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
12.50 ug/mL
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Positive EGFR expression (EGFR +++/++) | ||
| Method Description |
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
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| In Vitro Model | Lung large cell carcinoma | NCI-H1299 cells | CVCL_0060 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100.00 ug/mL | Negative EGFR expression (EGFR -) | ||
| Method Description |
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
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| In Vitro Model | Lung squamous cell carcinoma | NCI-H520 cells | CVCL_1566 | ||
References
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