Linker Information
General Information of This Linker
| Linker ID |
LIN0MJVEZ
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| Linker Name |
Conjugate No.36 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 |
C17H25N3O8
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| Isosmiles |
O=C(N1CCC(NCCOCCOCCC(N[C@H](C)C(O)=O)=O)=O)C=CC1=O
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| InChI |
InChI=1S/C17H25N3O8/c1-12(17(25)26)19-14(22)5-8-27-10-11-28-9-6-18-13(21)4-7-20-15(23)2-3-16(20)24/h2-3,12H,4-11H2,1H3,(H,18,21)(H,19,22)(H,25,26)/t12-/m1/s1
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| InChIKey |
LAXYBBRBFDEYEV-GFCCVEGCSA-N
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| Pharmaceutical Properties |
Molecule Weight
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399.4
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Polar area
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151.34
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Complexity
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565.1595682
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xlogp Value
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-1.5697
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Heavy Count
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28
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Rot Bonds
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14
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Hbond acc
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7
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Hbond Donor
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3
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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.36 [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) |
0.4 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) |
1.5 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) |
2.55 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 | ||