Linker Information
General Information of This Linker
| Linker ID |
LIN0FNLNU
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| Linker Name |
Conjugate No.67 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 |
C25H37N5O6
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| Isosmiles |
CC(C)[C@H](NC(CCN1C(CCC1=O)=O)=O)C(N[C@@H](CCCCN)C(NC(C=C2)=CC=C2CO)=O)=O
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| InChI |
InChI=1S/C25H37N5O6/c1-16(2)23(29-20(32)12-14-30-21(33)10-11-22(30)34)25(36)28-19(5-3-4-13-26)24(35)27-18-8-6-17(15-31)7-9-18/h6-9,16,19,23,31H,3-5,10-15,26H2,1-2H3,(H,27,35)(H,28,36)(H,29,32)/t19-,23-/m0/s1
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| InChIKey |
CCOXHWAULVFYQK-CVDCTZTESA-N
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| Pharmaceutical Properties |
Molecule Weight
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503.6
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Polar area
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170.93
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Complexity
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874.4709303
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xlogp Value
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0.4111
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Heavy Count
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36
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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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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.67 [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) |
300 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 | ||