Linker Information
General Information of This Linker
| Linker ID |
LIN0UKVPM
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|---|---|---|---|---|---|---|
| Linker Name |
DBCO-4,6 nnAA-PEG-VKG
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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 |
C68H106N6O20
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| Isosmiles |
CC([C@H](NC(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(N(CC1)CCC21CC(C(NCCC(N3CC4=C(C#CC5=C3C=CC=C5)C=CC=C4)=O)=O)C2)=O)=O)C(N[C@@H](CCCCN)C(O)=O)=O)C
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| InChI |
InChI=1S/C68H106N6O20/c1-54(2)64(66(79)71-59(67(80)81)12-7-8-21-69)72-61(75)17-25-82-27-29-84-31-33-86-35-37-88-39-41-90-43-45-92-47-49-94-50-48-93-46-44-91-42-40-89-38-36-87-34-32-85-30-28-83-26-18-62(76)73-23-19-68(20-24-73)51-58(52-68)65(78)70-22-16-63(77)74-53-57-11-4-3-9-55(57)14-15-56-10-5-6-13-60(56)74/h3-6,9-11,13,54,58-59,64H,7-8,12,16-53,69H2,1-2H3,(H,70,78)(H,71,79)(H,72,75)(H,80,81)/t59-,64-/m0/s1
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| InChIKey |
MEUSASQZMZPZGK-CQEHKKIPSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1327.618
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Polar area
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311.23
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Complexity
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2419.838437
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xlogp Value
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3.2933
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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
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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-Y180F404/K42/E161-LP15 [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) |
0.018 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-Yl80F404/K42/E161- LP15 [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) |
0.018 nM
|
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