Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0YLQTQ
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| ADC Name |
n501-MMAE
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| Synonyms |
n501-MMAE
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| Organization |
Fudan University; Hebei Agricultural University.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
0.88
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| Structure |
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| Antibody Name |
n501
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Antibody Info | ||||
| Antigen Name |
Trophoblast glycoprotein (TPBG)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Mc-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteine.
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| Combination Type |
Vedotin
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General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Maximum Observed Concentration (Cmax) | 44.9±7.4 | ug/mL |
Pharmacokinetic parameters of ADC in Healthy BALB/c mice.
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[1] |
| Maximum Observed Concentration (Cmax) | 27.89±9.04 | ug/mL |
Pharmacokinetic parameters of ADC in BxPC-3 xenograft nude mice
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[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Elimination Half-Life (t1/2) | 1.68±0.11 | h |
Pharmacokinetic parameters of ADC in Healthy BALB/c mice.
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[1] |
| Elimination Half-Life (t1/2) | 2.69±0.59 | h |
Pharmacokinetic parameters of ADC in BxPC-3 xenograft nude mice
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[1] |
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 14.27 nM | Moderate 5T4 expression (5T4++) | ||
| Method Description |
Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.
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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 inhibitory Concentration (lC50) | 16.32 nM | Moderate 5T4 expression (5T4++) | ||
| Method Description |
Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.
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| In Vitro Model | Ovarian mixed germ cell tumor | PA-1 cells | CVCL_0479 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 46.71 nM | High 5T4 expression (5T4 +++) | ||
| Method Description |
Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 51.22 nM | High 5T4 expression (5T4 +++) | ||
| Method Description |
Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 61.98 nM | Moderate 5T4 expression (5T4++) | ||
| Method Description |
Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 1000 nM | High 5T4 expression (5T4 +++) | ||
| Method Description |
Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | PANC-1 cells | CVCL_0480 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 1000 nM | Low 5T4 expression (5T4+) | ||
| Method Description |
Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.
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| In Vitro Model | Normal | FCHO cells | CVCL_U424 | ||
References