Linker Information
General Information of This Linker
| Linker ID |
LIN0BWOGF
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| Linker Name |
DBCO-nAA-PEG13-VKG
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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 |
C70H110N6O20
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| Isosmiles |
O=C(N(CC1)CCC1(CC2)CCC2C(NCCC(N3CC4=C(C#CC5=C3C=CC=C5)C=CC=C4)=O)=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(N[C@@H](C(C)C)C(N[C@@H](CCCCN)C(O)=O)=O)=O
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| InChI |
InChI=1S/C70H110N6O20/c1-56(2)66(68(81)73-61(69(82)83)12-7-8-25-71)74-63(77)19-29-84-31-33-86-35-37-88-39-41-90-43-45-92-47-49-94-51-53-96-54-52-95-50-48-93-46-44-91-42-40-89-38-36-87-34-32-85-30-20-64(78)75-27-23-70(24-28-75)21-16-59(17-22-70)67(80)72-26-18-65(79)76-55-60-11-4-3-9-57(60)14-15-58-10-5-6-13-62(58)76/h3-6,9-11,13,56,59,61,66H,7-8,12,16-55,71H2,1-2H3,(H,72,80)(H,73,81)(H,74,77)(H,82,83)/t61-,66-/m0/s1
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| InChIKey |
ALMQBSUDYVWIRK-WXFHQJQRSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1355.672
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Polar area
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311.23
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Complexity
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2453.263696
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xlogp Value
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4.0735
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Heavy Count
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96
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Rot Bonds
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55
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Hbond acc
|
20
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Hbond Donor
|
5
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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-Y180/F404/K42/E161-LP7 [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) | > 10 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.
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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 | ||
IN202417103159A D04-Y180/F404/K42/E161-LP7 [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) | > 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 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10 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 | ||
References