Linker Information
General Information of This Linker
| Linker ID |
LIN0LLTOU
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| Linker Name |
H- (A114C)-#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 |
C29H42N8O6S
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| Isosmiles |
CC([C@H](NC(CCCCCNC(C(N=C1)=CN=C1S)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC2=CC=C(CO)C=C2)=O)=O)C
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| InChI |
InChI=1S/C29H42N8O6S/c1-18(2)25(37-23(39)8-4-3-5-13-31-26(40)22-15-34-24(44)16-33-22)28(42)36-21(7-6-14-32-29(30)43)27(41)35-20-11-9-19(17-38)10-12-20/h9-12,15-16,18,21,25,38H,3-8,13-14,17H2,1-2H3,(H,31,40)(H,34,44)(H,35,41)(H,36,42)(H,37,39)(H3,30,32,43)/t21-,25-/m0/s1
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| InChIKey |
CBYOOWSGBSFQDO-OFVILXPXSA-N
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| Pharmaceutical Properties |
Molecule Weight
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630.772
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Polar area
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217.53
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Complexity
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1183.604352
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xlogp Value
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1.2606
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Heavy Count
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44
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Rot Bonds
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18
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Hbond acc
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9
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Hbond Donor
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8
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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
H- (kK183C)-#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) |
15.7 ng/mL
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Positive Her2 expression (Her2+++/++) | ||
| Method Description |
Her2-Target expressing BT474 (breast cancer cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 13 concentrations.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
40.14 ng/mL
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Positive Her2 expression (Her2+++/++) | ||
| Method Description |
Her2-Target expressing (BT474 (breast cancer), N87 (gastric cancer), MDA-MB-361-DYT2 (breast cancer)) or Her2-non-expressing (MDA-MB-468, HT29) cells, or CD33-target expressing HL60, HEL92.1.7, NB4 or CD33-non-expressing (Raji) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 39 concentrations.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
593.62 ng/mL
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Positive Her2 expression (Her2+++/++) | ||
| Method Description |
Her2-Target expressing MDA-MB-361-DYT2 (breast cancer) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 39 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361-DYT2 cells | CVCL_0620 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
37019 ng/mL
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Negative Her2 expression (Her2-) | ||
| Method Description |
Her2-non-expressing HT29) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 31 concentrations.
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| In Vitro Model | Colon adenocarcinoma | HT29 cells (HER2-) | CVCL_0320 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
67418 ng/mL
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Negative Her2 expression (Her2-) | ||
| Method Description |
Her2-non-expressing (MDA-MB-468, HT29) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 34 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells (HER2-) | CVCL_0419 | ||
H- (A114C)-#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) |
39.08 ng/mL
|
Positive Her2 expression (Her2+++/++) | ||
| Method Description |
Her2-Target expressing BT474 (breast cancer cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 12 concentrations.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
82.68 ng/mL
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Positive Her2 expression (Her2+++/++) | ||
| Method Description |
Her2-Target expressing (BT474 (breast cancer), N87 (gastric cancer), MDA-MB-361-DYT2 (breast cancer)) or Her2-non-expressing (MDA-MB-468, HT29) cells, or CD33-target expressing HL60, HEL92.1.7, NB4 or CD33-non-expressing (Raji) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 38 concentrations.
Click to Show/Hide
|
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
409.53 ng/mL
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Positive Her2 expression (Her2+++/++) | ||
| Method Description |
Her2-Target expressing MDA-MB-361-DYT2 (breast cancer) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 38 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361-DYT2 cells | CVCL_0620 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
59931 ng/mL
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Negative Her2 expression (Her2-) | ||
| Method Description |
Her2-non-expressing (MDA-MB-468, HT29) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 33 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells (HER2-) | CVCL_0419 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
64944 ng/mL
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Negative Her2 expression (Her2-) | ||
| Method Description |
Her2-non-expressing HT29) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 31 concentrations.
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| In Vitro Model | Colon adenocarcinoma | HT29 cells (HER2-) | CVCL_0320 | ||
References