Linker Information
General Information of This Linker
| Linker ID |
LIN0FYBKF
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| Linker Name |
Conjugate No.38 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 |
C22H34N4O9
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| Isosmiles |
O=C(N1CCC(NCCOCCOCCC(N[C@@H](C(C)C)C(N[C@@H](C)C(O)=O)=O)=O)=O)C=CC1=O
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| InChI |
InChI=1S/C22H34N4O9/c1-14(2)20(21(31)24-15(3)22(32)33)25-17(28)7-10-34-12-13-35-11-8-23-16(27)6-9-26-18(29)4-5-19(26)30/h4-5,14-15,20H,6-13H2,1-3H3,(H,23,27)(H,24,31)(H,25,28)(H,32,33)/t15-,20-/m0/s1
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| InChIKey |
WRINQYZTAXZPIX-YWZLYKJASA-N
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| Pharmaceutical Properties |
Molecule Weight
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498.533
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Polar area
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180.44
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Complexity
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749.8600238
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xlogp Value
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-1.4289
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Heavy Count
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35
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Rot Bonds
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17
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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.38 [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) |
0.04 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) |
0.11 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) |
1.45 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 | ||