Linker Information
General Information of This Linker
| Linker ID |
LIN0DLNWW
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
DL18 linker
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C13H17N3O6
|
|||||
| Isosmiles |
C[C@H](NC([C@@H](NC(CCN1C(C=CC1=O)=O)=O)C)=O)C(O)=O
|
|||||
| PubChem CID | ||||||
| InChI |
InChI=1S/C13H17N3O6/c1-7(12(20)15-8(2)13(21)22)14-9(17)5-6-16-10(18)3-4-11(16)19/h3-4,7-8H,5-6H2,1-2H3,(H,14,17)(H,15,20)(H,21,22)/t7-,8-/m0/s1
|
|||||
| InChIKey |
BOSZKBSHBTUZTL-YUMQZZPRSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
311.294
|
Polar area
|
132.88
|
||
|
Complexity
|
494.1564001
|
xlogp Value
|
-1.6045
|
|||
|
Heavy Count
|
22
|
Rot Bonds
|
7
|
|||
|
Hbond acc
|
5
|
Hbond Donor
|
3
|
|||
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.86 [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
|
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.
|
||||
| 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) |
29.01 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.
|
||||
| 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) |
64.66 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.
|
||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||