Linker Information
General Information of This Linker
| Linker ID |
LIN0CCITI
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| Linker Name |
Conjugate No.122 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 |
C44H74N8O21
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| Isosmiles |
O=C(N1CCC(NCCOCCOCCC(N[C@@H](CCC(O)=O)C(NCC(NCC(NCC(NCC(NCCOCCOCCOCCOCCOCCOCCOCCOC)=O)=O)=O)=O)=O)=O)=O)C=CC1=O
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| InChI |
InChI=1S/C44H74N8O21/c1-64-14-15-68-20-21-70-24-25-72-28-29-73-27-26-71-23-22-69-19-18-67-13-9-46-37(55)30-47-38(56)31-48-39(57)32-49-40(58)33-50-44(63)34(2-5-43(61)62)51-36(54)7-11-65-16-17-66-12-8-45-35(53)6-10-52-41(59)3-4-42(52)60/h3-4,34H,2,5-33H2,1H3,(H,45,53)(H,46,55)(H,47,56)(H,48,57)(H,49,58)(H,50,63)(H,51,54)(H,61,62)/t34-/m0/s1
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| InChIKey |
NATOCROIWVDJOG-UMSFTDKQSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1051.111
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Polar area
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370.68
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Complexity
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1562.30376
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xlogp Value
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-5.4658
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Heavy Count
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73
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Rot Bonds
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49
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Hbond acc
|
20
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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
WO2019126691A1 Conjugate No.122 [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) |
0.02 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Lung adenocarcinoma | Calu3 cells | CVCL_0609 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.14 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Breast ductal carcinoma | JIMT1 cells | CVCL_2077 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1.37 nM
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Low HER2 expression (HER2+) | ||
| Method Description |
MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||