Linker Information
General Information of This Linker
| Linker ID |
LIN0SBXHD
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| Linker Name |
DBCO-PEG4-VA
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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 |
C38H50N4O10
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| Isosmiles |
CC([C@H](NC(CCOCCOCCOCCOCCNC(CCC(N1CC2=C(C#CC3=C1C=CC=C3)C=CC=C2)=O)=O)=O)C(N[C@@H](C)C(O)=O)=O)C
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| InChI |
InChI=1S/C38H50N4O10/c1-27(2)36(37(46)40-28(3)38(47)48)41-34(44)16-18-49-20-22-51-24-25-52-23-21-50-19-17-39-33(43)14-15-35(45)42-26-31-10-5-4-8-29(31)12-13-30-9-6-7-11-32(30)42/h4-11,27-28,36H,14-26H2,1-3H3,(H,39,43)(H,40,46)(H,41,44)(H,47,48)/t28-,36-/m0/s1
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| InChIKey |
NCRPBNJTZXMHMK-GOOPYHEFSA-N
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| Pharmaceutical Properties |
Molecule Weight
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722.836
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Polar area
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181.83
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Complexity
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1497.673149
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xlogp Value
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2.016
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Heavy Count
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52
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Rot Bonds
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23
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Hbond acc
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9
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Hbond Donor
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4
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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-LP9 [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) |
0.0003 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