Linker Information
General Information of This Linker
| Linker ID |
LIN0WVWSG
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| Linker Name |
DBCO-6,4 nnAA-B-Glucuronide-PEG12
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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 |
C76H110N6O26
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| Isosmiles |
COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(NC[C@H](NC(C(C1)CC21CCN(C(CCCCC(N3C4=C(C#CC5=C(C=CC=C5)C3)C=CC=C4)=O)=O)CC2)=O)C(NCCC(NCC6=CC(CO)=CC=C6O[C@H]7[C@H](O)[C@@H](O)[C@H](O)C(O7)C(O)=O)=O)=O)=O
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| InChI |
InChI=1S/C76H110N6O26/c1-95-26-27-97-30-31-99-34-35-101-38-39-103-42-43-105-46-47-106-45-44-104-41-40-102-37-36-100-33-32-98-29-28-96-25-19-65(85)79-52-61(73(92)77-22-18-64(84)78-51-59-48-55(54-83)14-17-63(59)107-75-70(90)68(88)69(89)71(108-75)74(93)94)80-72(91)60-49-76(50-60)20-23-81(24-21-76)66(86)12-6-7-13-67(87)82-53-58-10-3-2-8-56(58)15-16-57-9-4-5-11-62(57)82/h2-5,8-11,14,17,48,60-61,68-71,75,83,88-90H,6-7,12-13,18-47,49-54H2,1H3,(H,77,92)(H,78,84)(H,79,85)(H,80,91)(H,93,94)/t61-,68-,69-,70+,71?,75+/m0/s1
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| InChIKey |
SWNNQWFYYXZSEV-GTHHBDGSSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1523.732
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Polar area
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404.46
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Complexity
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3134.182682
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xlogp Value
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0.9183
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Heavy Count
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108
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Rot Bonds
|
55
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Hbond acc
|
25
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Hbond Donor
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9
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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-Y180F404/K42/E161-LP23 [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) |
0.108 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.
Click to Show/Hide
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
ZA202500202A D04-Y180F404/K42/E161-LP19 [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) |
0.236 nM
|
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.
Click to Show/Hide
|
||||
| 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.
Click to Show/Hide
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
References