Linker Information
General Information of This Linker
| Linker ID |
LIN0WENVS
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| Linker Name |
Conjugate No.71 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 |
C29H43N5O9
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| Isosmiles |
C[C@H](NC([C@@H](NC(CCOCCOCCNC(CCN1C(CCC1=O)=O)=O)=O)C(C)C)=O)C(NC(C=C2)=CC=C2CO)=O
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| InChI |
InChI=1S/C29H43N5O9/c1-19(2)27(29(41)31-20(3)28(40)32-22-6-4-21(18-35)5-7-22)33-24(37)11-14-42-16-17-43-15-12-30-23(36)10-13-34-25(38)8-9-26(34)39/h4-7,19-20,27,35H,8-18H2,1-3H3,(H,30,36)(H,31,41)(H,32,40)(H,33,37)/t20-,27-/m0/s1
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| InChIKey |
BTXWZOGHPUJSHT-DCFHFQCYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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605.689
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Polar area
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192.47
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Complexity
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1041.760458
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xlogp Value
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-0.1585
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Heavy Count
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43
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Rot Bonds
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19
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Hbond acc
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9
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Hbond Donor
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5
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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.71 [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) |
0.03 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) |
10.74 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 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
300 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 | ||