Linker Information
General Information of This Linker
| Linker ID |
LIN0REHOH
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| Linker Name |
P5- (PEG12)
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| Linker Type |
Uncleavable linker
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| Antibody-Linker Relation |
Uncleavable
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| Structure |
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| Formula |
C33H56NO16P
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| Isosmiles |
C#CP(NC1=CC=C(C(O)=O)C=C1)(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO)=O
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| InChI |
InChI=1S/C33H56NO16P/c1-2-51(38,34-32-5-3-31(4-6-32)33(36)37)50-30-29-49-28-27-48-26-25-47-24-23-46-22-21-45-20-19-44-18-17-43-16-15-42-14-13-41-12-11-40-10-9-39-8-7-35/h1,3-6,35H,7-30H2,(H,34,38)(H,36,37)
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| InChIKey |
CPMPADBZTNSLLW-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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753.776
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Polar area
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197.39
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Complexity
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970.2858391
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xlogp Value
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1.772
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Heavy Count
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51
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Rot Bonds
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39
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Hbond acc
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15
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Hbond Donor
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3
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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
37828728 ADC 8 [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) |
182.4 ng/mL
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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.).
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| 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.).
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| In Vitro Model | Lung adenocarcinoma | HCC-78 cells | CVCL_2061 | ||
References