Linker Information
General Information of This Linker
| Linker ID |
LIN0NNKCS
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| Linker Name |
H- (A114C)-#66 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 |
C27H35N5O11S
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| Isosmiles |
OC([C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@H](OC2=C(NC(CCNC(CCCCCNC(C3=CN=C(S)N=C3)=O)=O)=O)C=C(CO)C=C2)O1)=O
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| InChI |
InChI=1S/C27H35N5O11S/c33-13-14-5-6-17(42-26-22(38)20(36)21(37)23(43-26)25(40)41)16(10-14)32-19(35)7-9-28-18(34)4-2-1-3-8-29-24(39)15-11-30-27(44)31-12-15/h5-6,10-12,20-23,26,33,36-38H,1-4,7-9,13H2,(H,28,34)(H,29,39)(H,32,35)(H,40,41)(H,30,31,44)/t20-,21-,22+,23-,26+/m0/s1
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| InChIKey |
SQHVHJCLRDPDIX-FMLGWJCWSA-N
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| Pharmaceutical Properties |
Molecule Weight
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637.668
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Polar area
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249.76
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Complexity
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1237.299465
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xlogp Value
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-1.0362
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Heavy Count
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44
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Rot Bonds
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15
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Hbond acc
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13
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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)-#66 [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) |
21.7 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 16 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) |
69.18 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 46 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) |
455 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 46 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) |
18236 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) |
21644 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 36 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells (HER2-) | CVCL_0419 | ||
References