Linker Information
General Information of This Linker
| Linker ID |
LIN0EQWJK
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| Linker Name |
Conjugate No.73 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 |
C15H23N3O6S
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| Isosmiles |
C[C@H](NC([C@@H](NC(CCN1C(C(S)CC1=O)=O)=O)C(C)C)=O)C(O)=O
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| InChI |
InChI=1S/C15H23N3O6S/c1-7(2)12(13(21)16-8(3)15(23)24)17-10(19)4-5-18-11(20)6-9(25)14(18)22/h7-9,12,25H,4-6H2,1-3H3,(H,16,21)(H,17,19)(H,23,24)/t8-,9?,12-/m0/s1
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| InChIKey |
BEKZEUPYEPQKJB-OYGLUPDLSA-N
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| Pharmaceutical Properties |
Molecule Weight
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373.431
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Polar area
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132.88
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Complexity
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542.385619
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xlogp Value
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-0.8361
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Heavy Count
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25
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Rot Bonds
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8
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Hbond acc
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6
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Hbond Donor
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4
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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.73 [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
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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) |
24.18 nM
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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) |
30.6 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.73A [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) |
0.05 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
OVCAR3 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 | High grade ovarian serous adenocarcinoma | OVCAR3 cells | CVCL_0465 | ||