Linker Information
General Information of This Linker
| Linker ID |
LIN0SIEYA
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| Linker Name |
DBCO-6,6 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 |
C78H114N6O26
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| Isosmiles |
COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(NC[C@H](NC(C(CC1)CCC21CCN(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@H](O7)C(O)=O)=O)=O)=O
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| InChI |
InChI=1S/C78H114N6O26/c1-97-30-31-99-34-35-101-38-39-103-42-43-105-46-47-107-50-51-108-49-48-106-45-44-104-41-40-102-37-36-100-33-32-98-29-21-67(87)81-54-63(75(94)79-26-20-66(86)80-53-62-52-57(56-85)14-17-65(62)109-77-72(92)70(90)71(91)73(110-77)76(95)96)82-74(93)60-18-22-78(23-19-60)24-27-83(28-25-78)68(88)12-6-7-13-69(89)84-55-61-10-3-2-8-58(61)15-16-59-9-4-5-11-64(59)84/h2-5,8-11,14,17,52,60,63,70-73,77,85,90-92H,6-7,12-13,18-51,53-56H2,1H3,(H,79,94)(H,80,86)(H,81,87)(H,82,93)(H,95,96)/t63-,70-,71-,72+,73-,77+/m0/s1
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| InChIKey |
IVOWNIDLZGRGLB-DMKKAORXSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1551.786
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Polar area
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404.46
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Complexity
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3168.844671
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xlogp Value
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1.6985
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Heavy Count
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110
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Rot Bonds
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55
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Hbond acc
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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-LP18 [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) |
0.373 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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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
References