Linker Information
General Information of This Linker
| Linker ID |
LIN0RZAQZ
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| Linker Name |
DBCO-PEG4-AAN
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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 |
C40H52N6O12
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| Isosmiles |
C[C@H](NC(CCOCCOCCOCCOCCNC(CCC(N1CC2=C(C#CC3=C1C=CC=C3)C=CC=C2)=O)=O)=O)C(N[C@@H](C)C(N[C@H](C(O)=O)CC(N)=O)=O)=O
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| InChI |
InChI=1S/C40H52N6O12/c1-27(38(51)44-28(2)39(52)45-32(40(53)54)25-34(41)47)43-36(49)15-17-55-19-21-57-23-24-58-22-20-56-18-16-42-35(48)13-14-37(50)46-26-31-9-4-3-7-29(31)11-12-30-8-5-6-10-33(30)46/h3-10,27-28,32H,13-26H2,1-2H3,(H2,41,47)(H,42,48)(H,43,49)(H,44,51)(H,45,52)(H,53,54)/t27-,28-,32-/m0/s1
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| InChIKey |
ZXPIHXYQSNKOLP-HPSLPFNASA-N
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| Pharmaceutical Properties |
Molecule Weight
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808.886
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Polar area
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254.02
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Complexity
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1725.94099
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xlogp Value
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-0.2599
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Heavy Count
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58
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Rot Bonds
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26
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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 D04-F404-LP33 [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) |
0.01 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.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
References