Linker Information
General Information of This Linker
| Linker ID |
LIN0QZTTH
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| Linker Name |
DBCO-nnAA-PEG13-AAA
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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 |
C68H104N6O21
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| Isosmiles |
C[C@H](NC([C@@H](NC([C@@H](NC(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(N(CC1)CCC1(CC2)CCC2C(NCCC(N3CC4=C(C#CC5=C3C=CC=C5)C=CC=C4)=O)=O)=O)=O)C)=O)C)=O)C(O)=O
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| InChI |
InChI=1S/C68H104N6O21/c1-53(64(78)71-54(2)65(79)72-55(3)67(81)82)70-61(75)17-26-83-28-30-85-32-34-87-36-38-89-40-42-91-44-46-93-48-50-95-51-49-94-47-45-92-43-41-90-39-37-88-35-33-86-31-29-84-27-18-62(76)73-24-21-68(22-25-73)19-14-58(15-20-68)66(80)69-23-16-63(77)74-52-59-10-5-4-8-56(59)12-13-57-9-6-7-11-60(57)74/h4-11,53-55,58H,14-52H2,1-3H3,(H,69,80)(H,70,75)(H,71,78)(H,72,79)(H,81,82)/t53-,54-,55-/m0/s1
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| InChIKey |
FEAIJGVMNCXRKV-JAZQDMDPSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1341.601
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Polar area
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314.31
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Complexity
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2504.527527
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xlogp Value
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2.833
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Heavy Count
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95
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Rot Bonds
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52
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Hbond acc
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20
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Hbond Donor
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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-LP6 [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) |
0.028 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-Y180/F404/K42/E161-LP6 [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) |
0.028 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