Linker Information
General Information of This Linker
| Linker ID |
LIN0PHNFR
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|---|---|---|---|---|---|---|
| Linker Name |
Conjugate No.20 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 |
C50H88N8O24
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| Isosmiles |
OCC(NC(CNC(CNC(CNC(CNC(CCOCCOCCNC(CCN(C(C=C1)=O)C1=O)=O)=O)=O)=O)=O)=O)C(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O
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| InChI |
InChI=1S/C50H88N8O24/c1-69-12-13-73-18-19-75-22-23-77-26-27-79-30-31-81-34-35-82-33-32-80-29-28-78-25-24-76-21-20-74-17-16-72-11-7-52-50(68)41(40-59)57-47(65)39-56-46(64)38-55-45(63)37-54-44(62)36-53-43(61)5-9-70-14-15-71-10-6-51-42(60)4-8-58-48(66)2-3-49(58)67/h2-3,41,59H,4-40H2,1H3,(H,51,60)(H,52,68)(H,53,61)(H,54,62)(H,55,63)(H,56,64)(H,57,65)
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| InChIKey |
LHFYWHKRRPIFHB-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
|
1185.286
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Polar area
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390.53
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Complexity
|
1649.858568
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xlogp Value
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-6.2719
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Heavy Count
|
82
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Rot Bonds
|
59
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Hbond acc
|
24
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Hbond Donor
|
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.20 [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) |
0.26 nM
|
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 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
300 nM
|
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 | ||
WO2019126691A1 Conjugate No.31 [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) |
0.26 nM
|
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) |
1.35 nM
|
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) |
2.73 nM
|
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 | ||