Linker Information
General Information of This Linker
| Linker ID |
LIN0OVFHQ
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| Linker Name |
DBCO-bridged nnAA-PEG-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 |
C68H105N7O21
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| Isosmiles |
CC([C@H](NC(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(NCC1(C2)CC2(C(NCCC(N3CC4=C(C#CC5=C3C=CC=C5)C=CC=C4)=O)=O)C1)=O)=O)C(N[C@@H](CCCCN)C(NCC(O)=O)=O)=O)C
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| InChI |
InChI=1S/C68H105N7O21/c1-53(2)63(65(82)73-57(12-7-8-19-69)64(81)71-47-62(79)80)74-60(77)18-22-85-24-26-87-28-30-89-32-34-91-36-38-93-40-42-95-44-46-96-45-43-94-41-39-92-37-35-90-33-31-88-29-27-86-25-23-84-21-17-59(76)72-52-67-49-68(50-67,51-67)66(83)70-20-16-61(78)75-48-56-11-4-3-9-54(56)14-15-55-10-5-6-13-58(55)75/h3-6,9-11,13,53,57,63H,7-8,12,16-52,69H2,1-2H3,(H,70,83)(H,71,81)(H,72,76)(H,73,82)(H,74,77)(H,79,80)/t57-,63-,67?,68?/m0/s1
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| InChIKey |
XLTGFBRHSTUTNV-ZDUFIGGCSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1356.616
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Polar area
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349.12
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Complexity
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2534.345147
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xlogp Value
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1.6772
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Heavy Count
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96
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Rot Bonds
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59
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Hbond acc
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21
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Hbond Donor
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7
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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-LP17 [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) |
0.019 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.
Click to Show/Hide
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
IN202417103159A D04-Yl80F404/K42/E161-LP17 [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) |
0.019 nM
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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