Linker Information
General Information of This Linker
| Linker ID |
LIN0GXOUX
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| Linker Name |
DBCO sidechain PEG12 ValLys-pAB
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| Linker Type |
Unclear
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C68H103N7O19
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| Isosmiles |
COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(NC[C@H](NC(CCCCC(N1CC2=C(C#CC3=C1C=CC=C3)C=CC=C2)=O)=O)C(N[C@H](C(C)C)C(N[C@H](C(NC4=CC=C(CO)C=C4)=O)CCCCN)=O)=O)=O
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| InChI |
InChI=1S/C68H103N7O19/c1-53(2)65(68(82)73-59(15-10-11-26-69)66(80)71-58-23-19-54(52-76)20-24-58)74-67(81)60(72-63(78)17-8-9-18-64(79)75-51-57-14-5-4-12-55(57)21-22-56-13-6-7-16-61(56)75)50-70-62(77)25-27-84-30-31-86-34-35-88-38-39-90-42-43-92-46-47-94-49-48-93-45-44-91-41-40-89-37-36-87-33-32-85-29-28-83-3/h4-7,12-14,16,19-20,23-24,53,59-60,65,76H,8-11,15,17-18,25-52,69H2,1-3H3,(H,70,77)(H,71,80)(H,72,78)(H,73,82)(H,74,81)/t59-,60-,65+/m0/s1
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| InChIKey |
FKHLTTVOEMJGCK-PLPDYVAUSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1322.602
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Polar area
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322.82
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Complexity
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2542.113577
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xlogp Value
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3.1991
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Heavy Count
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94
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Rot Bonds
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56
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Hbond acc
|
20
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Hbond Donor
|
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-Y180/F404/K42/E161-LP12 [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) |
0.036 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 | ||
IN202417103159A D04-Y180/F404/K42/E161-LP12 [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) |
0.036 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