Linker Information
General Information of This Linker
| Linker ID |
LIN0VYOTL
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| Linker Name |
TE-VC-PAB
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C23H35N5O6S
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| Isosmiles |
CC([C@H](NC(CCCC(S)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(CO)C=C1)=O)=O)C
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| InChI |
InChI=1S/C23H35N5O6S/c1-14(2)20(28-18(30)6-3-7-19(31)35)22(33)27-17(5-4-12-25-23(24)34)21(32)26-16-10-8-15(13-29)9-11-16/h8-11,14,17,20,29H,3-7,12-13H2,1-2H3,(H,26,32)(H,27,33)(H,28,30)(H,31,35)(H3,24,25,34)/t17-,20-/m0/s1
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| InChIKey |
LMEVHJSRYWJFPR-PXNSSMCTSA-N
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| Pharmaceutical Properties |
Molecule Weight
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509.629
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Polar area
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179.72
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Complexity
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829.2942158
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xlogp Value
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0.8182
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Heavy Count
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35
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Rot Bonds
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15
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Hbond acc
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6
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Hbond Donor
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7
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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
40151029 ADC 2 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.085 nM
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Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.182 nM
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Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
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| In Vitro Model | Lung papillary adenocarcinoma | NCI-H441 cells | CVCL_1561 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.265 nM
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Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
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| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.418 nM
|
Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
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| In Vitro Model | Hypopharyngeal squamous cell carcinoma | FaDu cells | CVCL_1218 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1.945 nM
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Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
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| In Vitro Model | Breast acantholytic squamous cell carcinoma | HCC-1806 cells | CVCL_1258 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Negative TROP2 expression (TROP2-) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
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| In Vitro Model | Lung adenocarcinoma | Calu-6 cells | CVCL_0236 | ||
40151029 ADC 1 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.144 nM
|
Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.224 nM
|
Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
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| In Vitro Model | Lung papillary adenocarcinoma | NCI-H441 cells | CVCL_1561 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.338 nM
|
Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.683 nM
|
Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
||||
| In Vitro Model | Hypopharyngeal squamous cell carcinoma | FaDu cells | CVCL_1218 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1.027 nM
|
Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
|
||||
| In Vitro Model | Breast acantholytic squamous cell carcinoma | HCC-1806 cells | CVCL_1258 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Negative TROP2 expression (TROP2-) | ||
| Method Description |
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.
Click to Show/Hide
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| In Vitro Model | Lung adenocarcinoma | Calu-6 cells | CVCL_0236 | ||
References
