Linker Information
General Information of This Linker
| Linker ID |
LIN0QQSRF
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| Linker Name |
Conjugate No.79 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 |
C24H36N4O11
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| Isosmiles |
C[C@H](NC([C@@H](NC([C@H](CCC(NCCOCCOCCC(O)=O)=O)N1C(C=CC1=O)=O)=O)C(C)C)=O)C(O)=O
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| InChI |
InChI=1S/C24H36N4O11/c1-14(2)21(23(35)26-15(3)24(36)37)27-22(34)16(28-18(30)6-7-19(28)31)4-5-17(29)25-9-11-39-13-12-38-10-8-20(32)33/h6-7,14-16,21H,4-5,8-13H2,1-3H3,(H,25,29)(H,26,35)(H,27,34)(H,32,33)(H,36,37)/t15-,16-,21-/m0/s1
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| InChIKey |
SLOYDYVMVMAYGJ-QYWGDWMGSA-N
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| Pharmaceutical Properties |
Molecule Weight
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556.569
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Polar area
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217.74
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Complexity
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882.3228036
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xlogp Value
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-1.5856
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Heavy Count
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39
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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.79 [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) |
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 | ||