Linker Information
General Information of This Linker
| Linker ID |
LIN0HPXKH
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| Linker Name |
DBCO-nnAA-sidechain PEG12
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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 |
C60H93N5O16
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| Isosmiles |
COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(NC[C@H](N)C(N(CC1)CCC1(CC2)CCC2C(NCCCCC(N3CC4=C(C#CC5=C3C=CC=C5)C=CC=C4)=O)=O)=O)=O
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| InChI |
InChI=1S/C60H93N5O16/c1-70-26-27-72-30-31-74-34-35-76-38-39-78-42-43-80-46-47-81-45-44-79-41-40-77-37-36-75-33-32-73-29-28-71-25-17-56(66)63-48-54(61)59(69)64-23-20-60(21-24-64)18-15-52(16-19-60)58(68)62-22-7-6-12-57(67)65-49-53-10-3-2-8-50(53)13-14-51-9-4-5-11-55(51)65/h2-5,8-11,52,54H,6-7,12,15-49,61H2,1H3,(H,62,68)(H,63,66)/t54-/m0/s1
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| InChIKey |
XSHXPKKSCVZXCM-XSMLMOGHSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1140.423
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Polar area
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235.6
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Complexity
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2025.55924
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xlogp Value
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3.6811
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Heavy Count
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81
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Rot Bonds
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45
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Hbond acc
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17
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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-LP28 [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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|
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
IN202417103159A D04-F404-LP28 [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