Linker Information
General Information of This Linker
| Linker ID |
LIN0ZXXPD
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| Linker Name |
P5 (PEG24)-VC-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 |
C75H131N6O31P
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| Isosmiles |
CC([C@H](NC(C1=CC=C(NP(C#C)(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO)=O)C=C1)=O)C(N[C@@H](CCCNC(N)=O)C(NC2=CC=C(CO)C=C2)=O)=O)C
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| InChI |
InChI=1S/C75H131N6O31P/c1-4-113(88,81-69-13-9-67(10-14-69)72(84)80-71(65(2)3)74(86)79-70(6-5-15-77-75(76)87)73(85)78-68-11-7-66(64-83)8-12-68)112-63-62-111-61-60-110-59-58-109-57-56-108-55-54-107-53-52-106-51-50-105-49-48-104-47-46-103-45-44-102-43-42-101-41-40-100-39-38-99-37-36-98-35-34-97-33-32-96-31-30-95-29-28-94-27-26-93-25-24-92-23-22-91-21-20-90-19-18-89-17-16-82/h1,7-14,65,70-71,82-83H,5-6,15-64H2,2-3H3,(H,78,85)(H,79,86)(H,80,84)(H,81,88)(H3,76,77,87)/t70-,71-,113?/m0/s1
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| InChIKey |
PLVBDTJIUHDXIM-LTZMSPKPSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1643.858
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Polar area
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433.5
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Complexity
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2481.011142
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xlogp Value
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2.0917
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Heavy Count
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113
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Rot Bonds
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86
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Hbond acc
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31
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Hbond Donor
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8
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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 5 [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) |
12.5 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) |
97.6 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