Linker Information
General Information of This Linker
| Linker ID |
LIN0UJVWG
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| Linker Name |
Conjugate No.5 Linker
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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 |
C42H74N8O20
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| Isosmiles |
COCCOCCOCCOCCOCCOCCOCCOCCNC(C(NC(CNC(CNC(CNC(CNC(CCOCCOCCNC(CCN1C(CCC1=O)=O)=O)=O)=O)=O)=O)=O)CO)=O
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| InChI |
InChI=1S/C42H74N8O20/c1-61-12-13-65-18-19-67-22-23-69-26-27-70-25-24-68-21-20-66-17-16-64-11-7-44-42(60)33(32-51)49-39(57)31-48-38(56)30-47-37(55)29-46-36(54)28-45-35(53)5-9-62-14-15-63-10-6-43-34(52)4-8-50-40(58)2-3-41(50)59/h33,51H,2-32H2,1H3,(H,43,52)(H,44,60)(H,45,53)(H,46,54)(H,47,55)(H,48,56)(H,49,57)
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| InChIKey |
JLBONEJEPWNLAZ-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1011.09
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Polar area
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353.61
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Complexity
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1407.0557
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xlogp Value
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-6.1143
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Heavy Count
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70
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Rot Bonds
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47
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Hbond acc
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20
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Hbond Donor
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8
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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
WO2019126691A1 Conjugate No.60 [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) |
0.01 nM
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Lung adenocarcinoma | Calu3 cells | CVCL_0609 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.02 nM
|
Low HER2 expression (HER2+) | ||
| Method Description |
MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.11 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Breast ductal carcinoma | JIMT1 cells | CVCL_2077 | ||
WO2019126691A1 Conjugate No.61 [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) |
0.02 nM
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
HT29 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.21 nM
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
DLD1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Colon adenocarcinoma | DLD1 cells | CVCL_0248 | ||
WO2019126691A1 Conjugate No.10 [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) |
0.25 nM
|
Moderate HER2 expression (HER2++) | ||
| Method Description |
JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Breast ductal carcinoma | JIMT1 cells | CVCL_2077 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
10.1 nM
|
Low HER2 expression (HER2+) | ||
| Method Description |
MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
WO2019126691A1 Conjugate No.62 [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) |
1.37 nM
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
HT29 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1.72 nM
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
DLD1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Colon adenocarcinoma | DLD1 cells | CVCL_0248 | ||
WO2019126691A1 Conjugate No.5 [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) |
34 nM
|
Moderate HER2 expression (HER2++) | ||
| Method Description |
JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Breast ductal carcinoma | JIMT1 cells | CVCL_2077 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
300 nM
|
Low HER2 expression (HER2+) | ||
| Method Description |
MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||