General Information of This Linker
Linker ID
LIN0CJXEN
Linker Name
DBCO-nnAA-PEG13-VKG
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C72H113N7O21
Isosmiles
CC([C@H](NC(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(N(CC1)CCC1(CC2)CCC2C(NCCC(N3CC4=C(C#CC5=C3C=CC=C5)C=CC=C4)=O)=O)=O)=O)C(N[C@@H](CCCCN)C(NCC(O)=O)=O)=O)C
InChI
InChI=1S/C72H113N7O21/c1-57(2)68(71(87)76-62(12-7-8-25-73)70(86)75-55-67(83)84)77-64(80)19-29-88-31-33-90-35-37-92-39-41-94-43-45-96-47-49-98-51-53-100-54-52-99-50-48-97-46-44-95-42-40-93-38-36-91-34-32-89-30-20-65(81)78-27-23-72(24-28-78)21-16-60(17-22-72)69(85)74-26-18-66(82)79-56-61-11-4-3-9-58(61)14-15-59-10-5-6-13-63(59)79/h3-6,9-11,13,57,60,62,68H,7-8,12,16-56,73H2,1-2H3,(H,74,85)(H,75,86)(H,76,87)(H,77,80)(H,83,84)/t62-,68-/m0/s1
InChIKey
HXTOSNOEOQXUEJ-JUEFVQERSA-N
Pharmaceutical Properties
Molecule Weight
1412.724
Polar area
340.33
Complexity
2591.630053
xlogp Value
3.1897
Heavy Count
100
Rot Bonds
57
Hbond acc
21
Hbond Donor
6
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-LP4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.003 nM
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.

   Click to Show/Hide
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.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
IN202417103159A D04-Yl80/F404/K42/E161-LP4 8 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.003 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
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
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-Y180/F404/K42/E161-LP4 (8) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.004 nM
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.

   Click to Show/Hide
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.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
IN202417103159A D04-Y180/F404/K42/E161-LP4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.004 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
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
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-Y180/F241/F404/K42-LP4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.005 nM
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.

   Click to Show/Hide
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.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
IN202417103159A D04-Yl80/F241/F404/K42-LP4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.005 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
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
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-Y180F404/K42/E161-LP4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.013 nM
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.

   Click to Show/Hide
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.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-Y180/F404/K42/E161-LP4 (7.52) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.019 nM
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.

   Click to Show/Hide
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.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
IN202417103159A D04-Yl80/F404/K42/E161-LP4 7.52 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.019 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
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
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-Y180F404/K42/E161-LP21 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.076 nM
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.

   Click to Show/Hide
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.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
IN202417103159A D04-Yl80F404/K42/E161-LP21 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.076 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
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
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A AGFP-Y180/F241/F404/K42-LP4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM 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.

   Click to Show/Hide
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.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
IN202417103159A aGFP-Y180/F241/F404/K42-LP4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 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
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 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
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
References
Ref 1 Anti-ROR1 antibodies and antibody conjugates, compositions comprising Anti-ROR1 antibodies or antibody conjugates, and methods of making and using Anti-ROR1 antibodies and antibody conjugates
Ref 2 Anti-ROR1 antibodies and antibody conjugates, compositions comprising Anti-ROR1 antibodies or antibody conjugates, and methods of making and using Anti-ROR1 antibodies and antibody conjugates