Linker Information
General Information of This Linker
| Linker ID |
LIN0IPKWK
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
DBCO-L-Cysteic acid-PEG4 (OH)
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C30H37N3O10S
|
|||||
| Isosmiles |
O=C(N[C@@H](CS(=O)(O)=O)C(NCCC(N1CC2=C(C#CC3=C1C=CC=C3)C=CC=C2)=O)=O)CCOCCOCCOCCO
|
|||||
| InChI |
InChI=1S/C30H37N3O10S/c34-14-16-42-18-20-43-19-17-41-15-12-28(35)32-26(22-44(38,39)40)30(37)31-13-11-29(36)33-21-25-7-2-1-5-23(25)9-10-24-6-3-4-8-27(24)33/h1-8,26,34H,11-22H2,(H,31,37)(H,32,35)(H,38,39,40)/t26-/m0/s1
|
|||||
| InChIKey |
JZKMDCIRFFECCP-SANMLTNESA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
631.704
|
Polar area
|
180.8
|
||
|
Complexity
|
1382.752099
|
xlogp Value
|
0.2441
|
|||
|
Heavy Count
|
44
|
Rot Bonds
|
18
|
|||
|
Hbond acc
|
9
|
Hbond Donor
|
4
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
ZA202500202A D04-F404-LP31 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10 nM | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.
Click to Show/Hide
|
||||
| In Vitro Model | Embryonal carcinoma | Ntera-2 cells | CVCL_0034 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10 nM | Negative ROR1 expression (ROR1-) | ||
| Method Description |
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.
Click to Show/Hide
|
||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
IN202417103159A D04-F404-LP31 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10 nM | Negative ROR1 expression (ROR1-) | ||
| Method Description |
The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
|
||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10 nM | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
|
||||
| In Vitro Model | Embryonal carcinoma | Ntera-2 cells | CVCL_0034 | ||
References