Linker Information
General Information of This Linker
| Linker ID |
LIN0UYVUM
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|---|---|---|---|---|---|---|
| Linker Name |
DBCO-nnAA-sidechain PEG12-EDA
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| Linker Type |
Unclear
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C63H98N6O17
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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(NCCN)=O)=O
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| InChI |
InChI=1S/C63H98N6O17/c1-75-28-29-77-32-33-79-36-37-81-40-41-83-44-45-85-48-49-86-47-46-84-43-42-82-39-38-80-35-34-78-31-30-76-27-18-58(70)66-50-56(62(74)65-24-23-64)67-61(73)54-16-19-63(20-17-54)21-25-68(26-22-63)59(71)12-6-7-13-60(72)69-51-55-10-3-2-8-52(55)14-15-53-9-4-5-11-57(53)69/h2-5,8-11,54,56H,6-7,12-13,16-51,64H2,1H3,(H,65,74)(H,66,70)(H,67,73)/t56-/m0/s1
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| InChIKey |
MIAJJWKIFTYXFJ-UWGNJQTFSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1211.502
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Polar area
|
264.7
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Complexity
|
2177.815191
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xlogp Value
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3.1874
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Heavy Count
|
86
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Rot Bonds
|
48
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Hbond acc
|
18
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Hbond Donor
|
4
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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-LP27 [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) |
0.017 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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|
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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 | ||
IN202417103159A D04-F404-LP27 [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) |
0.017 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