General Information of This Linker
Linker ID
LIN0UUQIV
Linker Name
DBCO-L-Cysteic acid-PEG4-Gly
Linker Type
Unclear
Antibody-Linker Relation
Cleavable
Structure
Formula
C34H45N5O11S
Isosmiles
O=C(NCCC(N1C2=C(C#CC3=C(C=CC=C3)C1)C=CC=C2)=O)[C@@H](NC(CCOCCOCCOCCOCCNC(CN)=O)=O)CS(=O)(O)=O
InChI
InChI=1S/C34H45N5O11S/c35-23-32(41)36-14-16-48-18-20-50-22-21-49-19-17-47-15-12-31(40)38-29(25-51(44,45)46)34(43)37-13-11-33(42)39-24-28-7-2-1-5-26(28)9-10-27-6-3-4-8-30(27)39/h1-8,29H,11-25,35H2,(H,36,41)(H,37,43)(H,38,40)(H,44,45,46)/t29-/m0/s1
InChIKey
WBPYSZWFRJBERA-LJAQVGFWSA-N
Pharmaceutical Properties
Molecule Weight
731.825
Polar area
224.92
Complexity
1560.802648
xlogp Value
-0.6567
Heavy Count
51
Rot Bonds
23
Hbond acc
11
Hbond Donor
5
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
ZA202500202A D04-F404-LP32 [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)
2.955 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-F404-LP32 [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)
2.955 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-LP32 [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 D04-Yl80/F404-LP32 [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