Linker Information
General Information of This Linker
| Linker ID |
LIN0NNAXX
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| Linker Name |
Conjugate No.26 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 |
C20H30N4O9
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| Isosmiles |
C[C@H](NC(CCOCCOCCNC(CCN1C(C=CC1=O)=O)=O)=O)C(N[C@@H](C)C(O)=O)=O
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| InChI |
InChI=1S/C20H30N4O9/c1-13(19(29)23-14(2)20(30)31)22-16(26)6-9-32-11-12-33-10-7-21-15(25)5-8-24-17(27)3-4-18(24)28/h3-4,13-14H,5-12H2,1-2H3,(H,21,25)(H,22,26)(H,23,29)(H,30,31)/t13-,14-/m0/s1
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| InChIKey |
HZTNPMXWIGTXQV-KBPBESRZSA-N
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| Pharmaceutical Properties |
Molecule Weight
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470.479
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Polar area
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180.44
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Complexity
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707.1372704
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xlogp Value
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-2.065
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Heavy Count
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33
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Rot Bonds
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16
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Hbond acc
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8
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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.26 [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) |
0.07 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) |
0.2 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) |
2.15 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 | ||