Linker Information
General Information of This Linker
| Linker ID |
LIN0UKOSS
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| Linker Name |
H- (A114C)-#43 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 |
C28H39N9O7S
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| Isosmiles |
CC([C@H](NC([C@@H](NC(C)=O)CNC(C(C=N1)=CN=C1S)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC2=CC=C(C=C2)CO)=O)=O)C
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| InChI |
InChI=1S/C28H39N9O7S/c1-15(2)22(37-25(42)21(34-16(3)39)13-31-23(40)18-11-32-28(45)33-12-18)26(43)36-20(5-4-10-30-27(29)44)24(41)35-19-8-6-17(14-38)7-9-19/h6-9,11-12,15,20-22,38H,4-5,10,13-14H2,1-3H3,(H,31,40)(H,34,39)(H,35,41)(H,36,43)(H,37,42)(H3,29,30,44)(H,32,33,45)/t20-,21-,22-/m0/s1
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| InChIKey |
GJMJLQYDDMGWPD-FKBYEOEOSA-N
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| Pharmaceutical Properties |
Molecule Weight
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645.743
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Polar area
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246.63
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Complexity
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1276.553564
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xlogp Value
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-0.7951
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Heavy Count
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45
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Rot Bonds
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16
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Hbond acc
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10
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Hbond Donor
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9
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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- (A114C)-#43 [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) |
16.6 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 15 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) |
22.75 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 42 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361-DYT2 cells | CVCL_0620 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
33.67 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 42 concentrations.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
27311 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 | ||
H- (A114C)-#52 [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) |
38.9 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 44 concentrations.
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|
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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) |
213.48 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 44 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361-DYT2 cells | CVCL_0620 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
24447 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 | ||
H- (A114C)-#46 [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) |
42.9 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 43 concentrations.
Click to Show/Hide
|
||||
| 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) |
461 ng/mL
|
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 43 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361-DYT2 cells | CVCL_0620 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
12465 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 | ||
H- (A114C)-#58 [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) |
734 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 45 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361-DYT2 cells | CVCL_0620 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1433 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 45 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) | > 60000 ng/mL | 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