Linker Information
General Information of This Linker
| Linker ID |
LIN0DUKKU
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| Linker Name |
DBCO-nnAA-PEG4-Gly
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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 |
C42H57N5O8
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| Isosmiles |
O=C(N1CC2=C(C#CC3=C1C=CC=C3)C=CC=C2)CCNC(C4CCC5(CC4)CCN(CC5)C(CCOCCOCCOCCOCCNC(CN)=O)=O)=O
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| InChI |
InChI=1S/C42H57N5O8/c43-31-38(48)44-20-24-53-26-28-55-30-29-54-27-25-52-23-14-39(49)46-21-17-42(18-22-46)15-11-35(12-16-42)41(51)45-19-13-40(50)47-32-36-7-2-1-5-33(36)9-10-34-6-3-4-8-37(34)47/h1-8,35H,11-32,43H2,(H,44,48)(H,45,51)
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| InChIKey |
SOIDUZGQKTVLCZ-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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759.945
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Polar area
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161.76
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Complexity
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1566.802648
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xlogp Value
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2.7697
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Heavy Count
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55
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Rot Bonds
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20
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Hbond acc
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9
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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
ZA202500202A D04-F404-LP25 [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) |
0.075 nM
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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.
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| 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.
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|
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
IN202417103159A D04-F404-LP25 [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) |
0.075 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
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| In Vitro Model | Embryonal carcinoma | Ntera-2 cells | CVCL_0034 | ||
| Experiment 2 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
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
References