Linker Information
General Information of This Linker
| Linker ID |
LIN0JQYIR
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| Linker Name |
DBCO-PEG4-GGFG-aminol
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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 |
C45H54N6O12
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| Isosmiles |
O=C(N1CC2=C(C#CC3=C1C=CC=C3)C=CC=C2)CCC(NCCOCCOCCOCCOCCC(NCC(NCC(N[C@@H](CC4=CC=CC=C4)C(NCC(O)=O)=O)=O)=O)=O)=O
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| InChI |
InChI=1S/C45H54N6O12/c52-39(16-17-43(56)51-32-36-12-5-4-10-34(36)14-15-35-11-6-7-13-38(35)51)46-19-21-61-23-25-63-27-26-62-24-22-60-20-18-40(53)47-29-41(54)48-30-42(55)50-37(45(59)49-31-44(57)58)28-33-8-2-1-3-9-33/h1-13,37H,16-32H2,(H,46,52)(H,47,53)(H,48,54)(H,49,59)(H,50,55)(H,57,58)/t37-/m0/s1
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| InChIKey |
NLAQYNJWFVJVOU-QNGWXLTQSA-N
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| Pharmaceutical Properties |
Molecule Weight
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870.957
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Polar area
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240.03
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Complexity
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1983.366
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xlogp Value
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0.4466
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Heavy Count
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63
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Rot Bonds
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28
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Hbond acc
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11
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Hbond Donor
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6
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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 2188-D04-Y180/F404/K42/E161-LP10 [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) |
0.048 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
|
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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
|
||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
IN202417103159A 2188-IN202417103159A D04-Yl80/F404/K42/E161 LP10 [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) |
0.048 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
|
||||
| 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 | ||
ZA202500202A 2188-D04-Y180/F404-LP10 [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) |
0.08 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
|
||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
IN202417103159A 2188-IN202417103159A D04-Yl80/F404-LP10 [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) |
0.08 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
|
||||
| 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