Linker ID	LIN0MASNF
Linker Name	DBCO-SO3-PEG4-Val-Cit-PABC
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
	3D MOL			2D MOL
Formula	C46H65N7O15S
Isosmiles	CC([C@H](NC(CCOCCOCCOCCOCCC(N[C@@H](CS(=O)(O)=O)C(NCCC(N1C2=C(C#CC3=C(C=CC=C3)C1)C=CC=C2)=O)=O)=O)=O)C(N[C@@H](CCCCN)C(NCC(O)=O)=O)=O)C
InChI	InChI=1S/C46H65N7O15S/c1-32(2)43(46(61)51-36(12-7-8-19-47)44(59)49-29-42(57)58)52-40(55)18-22-66-24-26-68-28-27-67-25-23-65-21-17-39(54)50-37(31-69(62,63)64)45(60)48-20-16-41(56)53-30-35-11-4-3-9-33(35)14-15-34-10-5-6-13-38(34)53/h3-6,9-11,13,32,36-37,43H,7-8,12,16-31,47H2,1-2H3,(H,48,60)(H,49,59)(H,50,54)(H,51,61)(H,52,55)(H,57,58)(H,62,63,64)/t36-,37-,43-/m0/s1
InChIKey	PIEUWURVNFJDEL-QJODFBJXSA-N
Pharmaceutical Properties	Molecule Weight		988.127	Polar area		320.42
	Complexity		2109.558438	xlogp Value		-0.3861
	Heavy Count		69	Rot Bonds		33
	Hbond acc		14	Hbond Donor		8

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.023 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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.05 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

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.05 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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.067 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

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.067 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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.082 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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.085 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

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.085 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

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

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

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

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