Linker Information
General Information of This Linker
| Linker ID |
LIN0VCWHG
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| Linker Name |
DBCO sidechain PEG12 ValGlu-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 |
C67H98N6O21
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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)CCC(O)=O)=O)=O)=O
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| InChI |
InChI=1S/C67H98N6O21/c1-51(2)64(67(82)71-57(22-23-63(78)79)65(80)69-56-20-16-52(50-74)17-21-56)72-66(81)58(70-61(76)14-8-9-15-62(77)73-49-55-12-5-4-10-53(55)18-19-54-11-6-7-13-59(54)73)48-68-60(75)24-25-84-28-29-86-32-33-88-36-37-90-40-41-92-44-45-94-47-46-93-43-42-91-39-38-89-35-34-87-31-30-85-27-26-83-3/h4-7,10-13,16-17,20-21,51,57-58,64,74H,8-9,14-15,22-50H2,1-3H3,(H,68,75)(H,69,80)(H,70,76)(H,71,82)(H,72,81)(H,78,79)/t57-,58-,64-/m0/s1
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| InChIKey |
SCKVMGISCIUPFW-XPSIIHHISA-N
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| Pharmaceutical Properties |
Molecule Weight
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1323.542
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Polar area
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334.1
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Complexity
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2609.541533
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xlogp Value
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2.9349
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Heavy Count
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94
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Rot Bonds
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55
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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-LP13 [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) |
0.072 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-LP13 [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) |
0.072 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