Linker Information
General Information of This Linker
| Linker ID |
LIN0VDOXW
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| Linker Name |
H- (A114C)-#30 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 |
C32H43N7O6S2
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| Isosmiles |
CC([C@H](NC(CCCCCNC(C1=CC=C(N=C(S)S2)C2=C1)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC3=CC=C(CO)C=C3)=O)=O)C
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| InChI |
InChI=1S/C32H43N7O6S2/c1-19(2)27(30(44)37-24(7-6-16-35-31(33)45)29(43)36-22-12-9-20(18-40)10-13-22)39-26(41)8-4-3-5-15-34-28(42)21-11-14-23-25(17-21)47-32(46)38-23/h9-14,17,19,24,27,40H,3-8,15-16,18H2,1-2H3,(H,34,42)(H,36,43)(H,37,44)(H,38,46)(H,39,41)(H3,33,35,45)/t24-,27-/m0/s1
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| InChIKey |
PEJHUDQJZBHUSH-IGKIAQTJSA-N
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| Pharmaceutical Properties |
Molecule Weight
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685.873
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Polar area
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204.64
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Complexity
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1465.968303
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xlogp Value
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3.0803
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Heavy Count
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47
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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- (A114C)-#30 [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) |
39.09 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 14 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) |
72.63 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 40 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) |
357.98 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 40 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) |
54582 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