Linker Information
General Information of This Linker
| Linker ID |
LIN0FYKUS
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| Linker Name |
P5 (PEG12)-VA-PAB
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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 |
C48H77N4O18P
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| Isosmiles |
CC([C@H](NC(C1=CC=C(NP(C#C)(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO)=O)C=C1)=O)C(N[C@@H](C)C(NC2=CC=C(CO)C=C2)=O)=O)C
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| InChI |
InChI=1S/C48H77N4O18P/c1-5-71(58,52-44-12-8-42(9-13-44)47(56)51-45(39(2)3)48(57)49-40(4)46(55)50-43-10-6-41(38-54)7-11-43)70-37-36-69-35-34-68-33-32-67-31-30-66-29-28-65-27-26-64-25-24-63-23-22-62-21-20-61-19-18-60-17-16-59-15-14-53/h1,6-13,39-40,45,53-54H,14-38H2,2-4H3,(H,49,57)(H,50,55)(H,51,56)(H,52,58)/t40-,45-,71?/m0/s1
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| InChIKey |
TXBCZOOMJPPLOQ-RMNYTVOVSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1029.128
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Polar area
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267.62
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Complexity
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1687.310495
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xlogp Value
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2.4639
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Heavy Count
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71
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Rot Bonds
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46
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Hbond acc
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18
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Hbond Donor
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6
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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 4 [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) |
18 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) |
121.2 ng/mL
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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