Linker Information
General Information of This Linker
| Linker ID |
LIN0NZTFN
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| Linker Name |
H- (A114C)-#35 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 |
C38H60N8O12S
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| Isosmiles |
CC([C@H](NC(CCOCCOCCOCCOCCOCCOCCNC(C1=CN=C(S)C=N1)=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/C38H60N8O12S/c1-27(2)34(37(51)45-30(4-3-10-41-38(39)52)36(50)44-29-7-5-28(26-47)6-8-29)46-32(48)9-12-53-14-16-55-18-20-57-22-23-58-21-19-56-17-15-54-13-11-40-35(49)31-24-43-33(59)25-42-31/h5-8,24-25,27,30,34,47H,3-4,9-23,26H2,1-2H3,(H,40,49)(H,43,59)(H,44,50)(H,45,51)(H,46,48)(H3,39,41,52)/t30-,34-/m0/s1
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| InChIKey |
ILVHVKSXDSPNSE-NHZFLZHXSA-N
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| Pharmaceutical Properties |
Molecule Weight
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853.009
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Polar area
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272.91
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Complexity
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1427.860821
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xlogp Value
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0.1899
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Heavy Count
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59
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Rot Bonds
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33
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Hbond acc
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15
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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)-#35 [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) |
36.79 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 41 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) |
75.18 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 41 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) |
18803 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 35 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells (HER2-) | CVCL_0419 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 63083 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