Linker Information
General Information of This Linker
| Linker ID |
LIN0FFEBZ
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
P5 (PEG12)-VA
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C41H70N3O18P
|
|||||
| Isosmiles |
CC([C@H](NC(C1=CC=C(NP(C#C)(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO)=O)C=C1)=O)C(N[C@@H](C)C(O)=O)=O)C
|
|||||
| InChI |
InChI=1S/C41H70N3O18P/c1-5-63(50,44-37-8-6-36(7-9-37)39(46)43-38(34(2)3)40(47)42-35(4)41(48)49)62-33-32-61-31-30-60-29-28-59-27-26-58-25-24-57-23-22-56-21-20-55-19-18-54-17-16-53-15-14-52-13-12-51-11-10-45/h1,6-9,34-35,38,45H,10-33H2,2-4H3,(H,42,47)(H,43,46)(H,44,50)(H,48,49)/t35-,38-,63?/m0/s1
|
|||||
| InChIKey |
VTHXTFOOFRZMSU-IWKFCSCDSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
923.988
|
Polar area
|
255.59
|
||
|
Complexity
|
1326.741059
|
xlogp Value
|
1.4175
|
|||
|
Heavy Count
|
63
|
Rot Bonds
|
44
|
|||
|
Hbond acc
|
17
|
Hbond Donor
|
5
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
37828728 ADC 7 [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) |
114.7 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).
Click to Show/Hide
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 3000 ng/mL | Negative HER2 expression (HER2-) | ||
| Method Description |
To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).
Click to Show/Hide
|
||||
| In Vitro Model | Lung adenocarcinoma | HCC-78 cells | CVCL_2061 | ||
References