Payload ID	PAY0UXDSB
Name	DX-8951 derivative (DXd)
Synonyms	1599440-33-1; Dxd; OQM5SD32BQ; N-[(10S,23S)-10-ethyl-18-fluoro-10-hydroxy-19-methyl-5,9-dioxo-8-oxa-4,15-diazahexacyclo[14.7.1.02,14.04,13.06,11.020,24]tetracosa-1,6(11),12,14,16,18,20(24)-heptaen-23-yl]-2-hydroxyacetamide; Exatecan derivative for ADC; Acetamide, N-((1S,9S)-9-ethyl-5-fluoro-2,3,9,10,13,15-hexahydro-9-hydroxy-4-methyl-10,13-dioxo-1H,12H-benzo(de)pyrano(3',4':6,7)indolizino(1,2-b)quinolin-1-yl)-2-hydroxy-; N-((1S,9S)-9-Ethyl-5-fluoro-2,3,9,10,13,15-hexahydro-9-hydroxy-4-methyl-10,13-dioxo-1H,12H-benzo(de)pyrano(3',4':6,7)indolizino(1,2-b)quinolin-1-yl)-2-hydroxyacetamide; N-((1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl)-2-hydroxyacetamide; N-[(1S,9S)-9-Ethyl-5-fluoro-2,3,9,10,13,15-hexahydro-9-hydroxy-4-methyl-10,13-dioxo-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl]-2-hydroxyacetamide; UNII-OQM5SD32BQ; SCHEMBL16485136; EX-A4319; HY-13631D; NSC825332; AT21797; NSC-825332; AC-32494; BP-27997; MS-29164; CS-0044752; A936339; N-[(10S,23S)-10-ethyl-18-fluoro-10-hydroxy-19-methyl-5,9-dioxo-8-oxa-4,15-diazahexacyclo[14.7.1.0,.0,.0,.0,tetracosa-1,6(11),12,14,16,18,20(24)-heptaen-23-yl]-2-hydroxyacetamide    Click to Show/Hide
Target	DNA topoisomerase 1 (TOP1)					Target Info
Structure
	3D MOL			2D MOL
Formula	C26H24FN3O6
Isosmiles	CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C5[C@H](CCC6=C5C(=CC(=C6C)F)N=C4C3=C2)NC(=O)CO)O
PubChem CID	117888634
InChI	InChI=1S/C26H24FN3O6/c1-3-26(35)15-6-19-23-13(8-30(19)24(33)14(15)10-36-25(26)34)22-17(28-20(32)9-31)5-4-12-11(2)16(27)7-18(29-23)21(12)22/h6-7,17,31,35H,3-5,8-10H2,1-2H3,(H,28,32)/t17-,26-/m0/s1
InChIKey	PLXLYXLUCNZSAA-QLXKLKPCSA-N
IUPAC Name	N-[(10S,23S)-10-ethyl-18-fluoro-10-hydroxy-19-methyl-5,9-dioxo-8-oxa-4,15-diazahexacyclo[14.7.1.02,14.04,13.06,11.020,24]tetracosa-1,6(11),12,14,16,18,20(24)-heptaen-23-yl]-2-hydroxyacetamide
Pharmaceutical Properties	Molecule Weight		493.5	Polar area		129
	Complexity		1080	xlogp Value		0
	Heavy Count		36	Rot Bonds		3
	Hbond acc		8	Hbond Donor		3

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	0.5	nM	MDA-MB-468 cells	Breast adenocarcinoma	CVCL_0419	[1]
Half Maximal Inhibitory Concentration (IC50)	4	nM	KPL-4 cells	Breast inflammatory carcinoma	CVCL_5310	[1]

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Negative CDH6 expression (CDH6-)
Method Description	The CDH6-negative human ovarian tumor cell line ES-2 was subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate H01L02-DXd was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model	ES-2 CDX model
In Vitro Model	Ovarian clear cell adenocarcinoma	ES-2 cells		CVCL_3509
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Negative CDH6 expression (CDH6-)
Method Description	The CDH6-negative human ovarian tumor cell line ES-2 was subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate H01L02-DXd was intravenously administered at doses of 1 mg/kg to thetail of each mouse.
In Vivo Model	ES-2 CDX model
In Vitro Model	Ovarian clear cell adenocarcinoma	ES-2 cells		CVCL_3509
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.87%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human renal cell tumor cell line786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 20 of grouping, the anti-body-drug conjugate H01L02-DXd was intravenously administered at doses of 1 mg/kg to thetail of each mouse.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75.34%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human renal cell tumor cell line786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 20 of grouping, the anti-body-drug conjugate H01L02-DXd was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 5 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 79.79%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human ovarian tumor cell line OVCAR-3 was subcutane-ously inoculated at a dose of 10,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 22 of grouping, theantibody-drug conjugate H01L02-DXd was intravenously administered at doses of 1 mg/kg to the tail of each mouse.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 6 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.25%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human renal cell tumor cell line 786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 18 of grouping, H01L02-DXd was intravenously administered at a dose of 3 mg/kg to the tail of each mouse.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 7 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.96%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human ovarian tumor cell line PA-1 was subcutaneously inoculatedat a dose of 8,500,000 cells to the right flank region of eachfemale nude mouse (Day 0). On the day 11 of grouping, the antibody-drug conjugate H01L02-DXd was intravenously administered at doses of 1 mg/kg to the tail of each mouse.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 8 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.76%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human ovarian tumor cell line OVCAR-3 was subcutane-ously inoculated at a dose of 10,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 22 of grouping, theantibody-drug conjugate H01L02-DXd was intravenously administered at doses of 3 mg/kg to the tail of each mouse.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 9 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.37%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human ovarian tumor cell line PA-1 was subcutaneously inoculatedat a dose of 8,500,000 cells to the right flank region of eachfemale nude mouse (Day 0). On the day 11 of grouping, the antibody-drug conjugate H01L02-DXd was intravenously administered at doses of 3 mg/kg to the tail of each mouse.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01-0.10 nM	Positive CDH6 expression (CDH6+++/++)
Method Description	CDH6-positive human ovarian tumor cell line PA-1 was seeded over a 96-well plate at 2,000 cells/100 L/well in MEM medium supplemented with 10% FBS, and the cells were then cultured overnight. On the next day, each of the 4 humanized hG019-drug conjugates or NOV0712-DM4 was added to the cells.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Low CD30 expression (CD30+)
Method Description	Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-DT=3 mg/kg.
In Vivo Model	HD CDX model
In Vitro Model	Hodgkin lymphoma	L-428 cells		CVCL_1361
Experiment 2 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Low CD30 expression (CD30+)
Method Description	Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-DT=1 mg/kg.
In Vivo Model	HD CDX model
In Vitro Model	Hodgkin lymphoma	L-428 cells		CVCL_1361
Experiment 3 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72%	Positive CD30 expression (CD30+++/++)
Method Description	Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-DT=3 mg/kg.
In Vivo Model	ALCL CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells/Karpas BVR cells		CVCL_1324
Experiment 4 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	Positive CD30 expression (CD30+++/++)
Method Description	Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-DT=10 mg/kg.
In Vivo Model	ALCL CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells/Karpas BVR cells		CVCL_1324
Experiment 5 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	High CD30 expression (CD30+++; 285,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	Precursor T-cell acute lymphoblastic leukemia	ALCL cells		CVCL_A036
Experiment 6 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16 ng/mL	High CD30 expression (CD30+++; 180,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	Anaplastic large cell lymphoma	DEL/BVR cells		CVCL_1170
Experiment 7 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26 ng/mL	High CD30 expression (CD30+++; 400,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Low CD30 expression (CD30+; 70,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	Hodgkin lymphoma	L-428 cells		CVCL_1361
Experiment 9 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	High CD30 expression (CD30+++; 320,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.20%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human ovarian tumor cell line PA-1 was subcutaneously inoculatedat a dose of 8,500,000 cells to the right flank region of eachfemale nude mouse (Day 0). On the day 11 of grouping, the antibody-drug conjugate NOV0712-DXd was intravenously administered at doses of 1 mg/kg to the tail of each mouse.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.12%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human ovarian tumor cell line PA-1 was subcutaneously inoculatedat a dose of 8,500,000 cells to the right flank region of eachfemale nude mouse (Day 0). On the day 11 of grouping, the antibody-drug conjugate NOV0712-DXd was intravenously administered at doses of 3 mg/kg to the tail of each mouse.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.59%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human renal cell tumor cell line 786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 18 of grouping, H02L03-DXd was intravenously administered at a dose of 3 mg/kg to the tail of each mouse.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive CDH6 expression (CDH6+++/++)
Method Description	CDH6-positive human ovarian tumor cell line PA-1 was seeded over a 96-well plate at 2,000 cells/100 L/well in MEM medium supplemented with 10% FBS, and the cells were then cultured overnight. On the next day, each of the 4 humanized hG019-drug conjugates or NOV0712-DM4 was added to the cells.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.53%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human renal cell tumor cell line 786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 18 of grouping, H04L02-DXd was intravenously administered at a dose of 3 mg/kg to the tail of each mouse.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10-1.00 nM	Positive CDH6 expression (CDH6+++/++)
Method Description	CDH6-positive human ovarian tumor cell line PA-1 was seeded over a 96-well plate at 2,000 cells/100 L/well in MEM medium supplemented with 10% FBS, and the cells were then cultured overnight. On the next day, each of the 4 humanized hG019-drug conjugates or NOV0712-DM4 was added to the cells.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92%	Positive CDH6 expression (CDH6+++/++)
Method Description	The CDH6-positive human renal cell tumor cell line 786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 18 of grouping, H02L02-DXd was intravenously administered at a dose of 3 mg/kg to the tail of each mouse.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01-0.10 nM	Positive CDH6 expression (CDH6+++/++)
Method Description	CDH6-positive human ovarian tumor cell line PA-1 was seeded over a 96-well plate at 2,000 cells/100 L/well in MEM medium supplemented with 10% FBS, and the cells were then cultured overnight. On the next day, each of the 4 humanized hG019-drug conjugates or NOV0712-DM4 was added to the cells.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	High CD30 expression (CD30+++; 180,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	Anaplastic large cell lymphoma	DEL/BVR cells		CVCL_1170
Experiment 2 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	High CD30 expression (CD30+++; 285,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	Precursor T-cell acute lymphoblastic leukemia	ALCL cells		CVCL_A036
Experiment 3 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Low CD30 expression (CD30+; 70,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	Hodgkin lymphoma	L-428 cells		CVCL_1361
Experiment 4 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	High CD30 expression (CD30+++; 320,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 5 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	High CD30 expression (CD30+++; 400,000 CD30 molecules/cell)
Method Description	Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.    Click to Show/Hide
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.32 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	70.36 nM	Moderate EGFR expression (EGFR++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	90.21 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative EGFR expression (EGFR-)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth lnhibition value (TGl)	72%	Positive TROP2 expression (TROP2+++/++)
Method Description	This PDX was obtained in accordance with appropriate consent procedures. This ovarian PDX model was subcutaneously passaged in vivo as fragments from animal to animal in nude mice. When tumors reached approximately 250 mm 3 similar-sized tumors were randomly assigned to treatment groups, DS-1062 was administered as a single dose at 10 mg/kg on day 1. Duration of dosing was 21 days. TGI responses (Day 28 TGI%) was measurede.    Click to Show/Hide
In Vivo Model	CTG-3718 human patient-derived xenograft (PDX) model
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth lnhibition value (TGl)	88%	Positive TROP2 expression (TROP2+++/++)
Method Description	Female Nude mice (Charles River) aged 5-8 weeks were used, following 7 days acclimatisation before entry into the study. The human patient-derived xenograft (PDX) model, CTG-3303, was established from fragments of freshly resected tumor of a triple negative breast cancer (TNBC) patient whom relapsed on treatment with PARP inhibitor talazoparib. This PDX was obtained in accordance with appropriate consent procedures. This TNBC PDX model was subcutaneously passaged in vivo as fragments from animal to animal in nude mice. When tumors reached approximately 250 mm 3 , similar-sized tumors were randomly assigned to treatment groups. DS-1062 was administered as a single dose at 10 mg/kg on day 1. Duration of dosing schedule was 21 days. TGI responses (Day 46 TGI%) was measurede.    Click to Show/Hide
In Vivo Model	CTG-3303 human patient-derived xenograft (PDX) model

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth lnhibition value (TGl)	82%	Positive TROP2 expression (TROP2+++/++)
Method Description	Nude mice (Charles River) aged 5-8 weeks wereused,following 7 days acclimatisation before entry intothe study.5x106 NCI-N87 tumor cells (gastric cancercell line) (1:1 in Matrigel)were implantedsubcutaneously onto the flank of the female Nude mice.When tumors reached approximately 250 mm,similar-sizedtumors were randomly assigned to treatment groups, DS-1062 was administered as a single dose at 10 mg/kg on day 1. Duration of dosing schedule was 21 days.    Click to Show/Hide
In Vivo Model	NCI-N87 Xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.009 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 30 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0572 nM	High Nectin-4 expression (Nectin-4 +++)
Method Description	Ab1 ADC was tested in T24 mScarlet clone 5 nectin-4 negative cells;and with a DAR of 8
In Vitro Model	Bladder carcinoma	T24 mScarlet clone 5 nectin-4 negative cells		CVCL_0554

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.075 nM	Positive ICAM-1 expression (ICAM-1+++/++)
Method Description	Cells from triple-negative breast cancer were propagated in slides with 96 chambers, each well containing 5000 cells. The medium was replaced with medium supplemented with nanoparticle Nab PTX, IgG-Dxd, or ICAM-1-Dxd at various concentrations. After 72 h, the toxic effects on the cells were assessed via a CCK-8 test. In brief, the medium containing the pharmaceuticals was discarded, and the cells were carefully rinsed with chilled PBS. The samples were subsequently incubated in a CCK-8 solution maintained at 37 °C for 4 h. The degree to which cell growth was suppressed was determined by comparing the optical density of agent-exposed cells to that of untreated control cells. In addition, extracellular ATP concentrations were quantified via a Beyotime ATP detection kit (S0026).    Click to Show/Hide
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.132 nM	Positive ICAM-1 expression (ICAM-1+++/++)
Method Description	Cells from triple-negative breast cancer were propagated in slides with 96 chambers, each well containing 5000 cells. The medium was replaced with medium supplemented with nanoparticle Nab PTX, IgG-Dxd, or ICAM-1-Dxd at various concentrations. After 72 h, the toxic effects on the cells were assessed via a CCK-8 test. In brief, the medium containing the pharmaceuticals was discarded, and the cells were carefully rinsed with chilled PBS. The samples were subsequently incubated in a CCK-8 solution maintained at 37 °C for 4 h. The degree to which cell growth was suppressed was determined by comparing the optical density of agent-exposed cells to that of untreated control cells. In addition, extracellular ATP concentrations were quantified via a Beyotime ATP detection kit (S0026).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.141 nM	Positive ICAM-1 expression (ICAM-1+++/++)
Method Description	Cells from triple-negative breast cancer were propagated in slides with 96 chambers, each well containing 5000 cells. The medium was replaced with medium supplemented with nanoparticle Nab PTX, IgG-Dxd, or ICAM-1-Dxd at various concentrations. After 72 h, the toxic effects on the cells were assessed via a CCK-8 test. In brief, the medium containing the pharmaceuticals was discarded, and the cells were carefully rinsed with chilled PBS. The samples were subsequently incubated in a CCK-8 solution maintained at 37 °C for 4 h. The degree to which cell growth was suppressed was determined by comparing the optical density of agent-exposed cells to that of untreated control cells. In addition, extracellular ATP concentrations were quantified via a Beyotime ATP detection kit (S0026).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	BT-549 cells		CVCL_1092

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.106 nM	High HER2 expression (HER2 +++)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.114 nM	High HER2 expression (HER2 +++)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.123 nM	High HER2 expression (HER2 +++)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.151 nM	High HER2 expression (HER2 +++)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.152 nM	High HER2 expression (HER2 +++)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.16 nM	High HER2 expression (HER2 +++)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.172 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well SK-BR-3 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well Calu-3 in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.73 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well NCI-N87 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Negative HER2 expression (HER2-)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 800/well NCI-H1975 cells in 80ul media (target negative cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.186 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well SK-BR-3 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.222 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well Calu-3 in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well NCI-N87 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Negative HER2 expression (HER2-)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 800/well NCI-H1975 cells in 80ul media (target negative cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.239 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Breast carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.892 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	UACC812 cells		CVCL_1781
Experiment 3 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.991 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.256 nM	High HER2 expression (HER2 +++)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.54&#1770.02 nM	Moderate TF expression (TF++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.39&#1770.47 nM	High TF expression (TF +++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low TF expression (TF+)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic adenocarcinoma	PSN-1 cells		CVCL_1644

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.55&#1770.20 nM	Moderate TF expression (TF++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.09&#1770.29 nM	High TF expression (TF +++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low TF expression (TF+)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic adenocarcinoma	PSN-1 cells		CVCL_1644

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.05 nM	Moderate SORT1 expression (SORT1++)
Method Description	The in vitro cell-killing assay was carried out using MDA-MB-231, MCF-7, MCF-10A, and T47D. Cells were plated in 96-well plates (5000 cells/well). After 1 h incubation, ADCs were added in a serial of concentrations with three replicates per concentration. The concentration of ADCs against MDA-MB-231, MCF-7, and MCF-10A ranged from 300 nM to 137 pM, while the range of concentration was from 100 nM to 46 pM for T47D. This was followed by another 72 h of culture. Cell viability was detected using the Cell Counting Kit 8 (APExBIO, Houston, TX, USA).    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	24.07 nM	Moderate SORT1 expression (SORT1++)
Method Description	The in vitro cell-killing assay was carried out using MDA-MB-231, MCF-7, MCF-10A, and T47D. Cells were plated in 96-well plates (5000 cells/well). After 1 h incubation, ADCs were added in a serial of concentrations with three replicates per concentration. The concentration of ADCs against MDA-MB-231, MCF-7, and MCF-10A ranged from 300 nM to 137 pM, while the range of concentration was from 100 nM to 46 pM for T47D. This was followed by another 72 h of culture. Cell viability was detected using the Cell Counting Kit 8 (APExBIO, Houston, TX, USA).    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.48&#1770.88 nM
Method Description	Human thyroid cancer cells were seeded in a 96-well plate at a density of 3000 cells per well overnight. The cell culture medium was replaced with the medium containing either chemo drugs (maximum concentration: 117.11 umol/L) or ICAM1-ADCs at serial diluted concentrations (maximum concentration: 0.67 umol/L). After 96h, cell cytotoxicity was determined by using a CCK-8 kit (KeyGEN Biotech, China) following the manufacturer's protocol. The absorbance at 450 nm was measured with an ELISA browser (Bio-Tek EL 800, USA). The experiments were repeated three times.    Click to Show/Hide
In Vitro Model	Differentiated thyroid carcinoma, Thyroid gland papillary carcinoma	IHH4 cells		CVCL_2960
Experiment 2 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	54.1&#17719.4 nM
Method Description	Human thyroid cancer cells were seeded in a 96-well plate at a density of 3000 cells per well overnight. The cell culture medium was replaced with the medium containing either chemo drugs (maximum concentration: 117.11 umol/L) or ICAM1-ADCs at serial diluted concentrations (maximum concentration: 0.67 umol/L). After 96h, cell cytotoxicity was determined by using a CCK-8 kit (KeyGEN Biotech, China) following the manufacturer's protocol. The absorbance at 450 nm was measured with an ELISA browser (Bio-Tek EL 800, USA). The experiments were repeated three times.    Click to Show/Hide
In Vitro Model	Thyroid carcinoma	BCPAP cells		CVCL_0153

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	11.4 nM	Low ID1 expression (ID1+)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.3 nM	Low ID1 expression (ID1+)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	80.71 nM	Negative HER expression (HER-)
Method Description	Using standard cell viability assay, the cytotoxicity and targeting specificity of ADC described in this paper were evaluated for her 2 positive SkBr-3 and her 2 negative MDA-MB-468 cancer cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Effective Concentration (EC50)	8.52 nM	Positive HER expression (HER+++/++)
Method Description	Using standard cell viability assay, the cytotoxicity and targeting specificity of ADC described in this paper were evaluated for her 2 positive SkBr-3 and her 2 negative MDA-MB-468 cancer cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	89.1 nM	Low ID1 expression (ID1+)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Moderate TF expression (TF++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	121 nM	Positive HER2expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well SK-BR-3 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	341 nM	Positive HER2expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well Calu-3 in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Positive HER2expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well NCI-N87 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Negative HER2 expression (HER2-)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 800/well NCI-H1975 cells in 80ul media (target negative cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	124.5 nM
Method Description	SHP-77 cells were grown in RPMI-1640 medium supplemented with 10% FBS and 1 ug/mL puromycin at 37 °C in a 5% CO2 incubator. SHP-77 cells were dissociated using TrypLETM Express Enzyme (Thermo Fisher Scientific, Waltham, MA, USA) and, after counting, the cells were resuspended in RPMI-1640 medium supplemented with 10% FBS at a density of 3 × 104 cells/mL. The cells were plated in 96-well plates and incubated at 37 °C for 24 h. ADCs and payloads were diluted separately and added to the 96-well cell culture plates containing cells, followed by incubation in a 5% CO2 incubator for 5 days. A multifunctional microplate reader was used, and the absorbance was measured at 450 nm with a reference wavelength of 630 nm. The IC50 values were calculated using GraphPad Prism 10.1.2 software.    Click to Show/Hide
In Vitro Model	Small cell lung carcinoma	SHP-77 cells		CVCL_1693

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	156 nM	Low ID1 expression (ID1+)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	212 nM	Positive HER2expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well SK-BR-3 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Positive HER2expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well NCI-N87 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Positive HER2expression (HER2+++/++)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well Calu-3 in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 4 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Negative HER2 expression (HER2-)
Method Description	Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 800/well NCI-H1975 cells in 80ul media (target negative cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Low ID1 expression (ID1+)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Low ID1 expression (ID1+)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 400 nM	Low ID1 expression (ID1+)
Method Description	The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144 hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1784 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.
Experiment 2 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3986 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2016 ng/mL	Negative CD138 expression (CD138-)
Method Description	1000 cells/well of Jurkat in 96 well, 37 °C for 5 days.
In Vitro Model	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10000 ng/mL	Positive CD138 expression (CD138+++/++)
Method Description	1000 cells/well of Capan-1 in 96 well, 37 °C for 5 days.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10000 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.
Experiment 2 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10000 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10000 ng/mL	Positive CD138 expression (CD138+++/++)
Method Description	1000 cells/well of Capan-1 in 96 well, 37 °C for 5 days.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10000 ng/mL	Negative CD138 expression (CD138-)
Method Description	1000 cells/well of Jurkat in 96 well, 37 °C for 5 days.
In Vitro Model	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5- 2 × 10 -5 ug/mL	Positive ASCT2 expression (ASCT2+++/++)
Method Description	Target cells were seeded in triplicates into flat-bottom 384-wells plate (400 cells for HCT116 cells). Cells were incubated for 3 to 4 hours at 37°C before addition of an equivalent volume of 2X concentrated ADC or free drug-linker dose range (see table 1 for details). Cells were then incubated into a live cell imaging instrument (Incucyte®) for 6 to 8 days and their confluency was monitored all along the culture.    Click to Show/Hide
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	135- 6.9 × 10 -3 g/mL	Positive ASCT2 expression (ASCT2+++/++)
Method Description	Target cells were seeded in triplicates into flat-bottom 384-wells plate (400 cells for HCT116 cells). Cells were incubated for 3 to 4 hours at 37°C before addition of an equivalent volume of 2X concentrated ADC or free drug-linker dose range (see table 1 for details). Cells were then incubated into a live cell imaging instrument (Incucyte®) for 6 to 8 days and their confluency was monitored all along the culture.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	WiDr cells		CVCL_2760

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5- 2 × 10 -5 ug/mL	Positive ASCT2 expression (ASCT2+++/++)
Method Description	Target cells were seeded in triplicates into flat-bottom 384-wells plate (400 cells for HCT116 cells). Cells were incubated for 3 to 4 hours at 37°C before addition of an equivalent volume of 2X concentrated ADC or free drug-linker dose range (see table 1 for details). Cells were then incubated into a live cell imaging instrument (Incucyte®) for 6 to 8 days and their confluency was monitored all along the culture.    Click to Show/Hide
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	135- 6.9 × 10 -3 g/mL	Positive ASCT2 expression (ASCT2+++/++)
Method Description	Target cells were seeded in triplicates into flat-bottom 384-wells plate (400 cells for HCT116 cells). Cells were incubated for 3 to 4 hours at 37°C before addition of an equivalent volume of 2X concentrated ADC or free drug-linker dose range (see table 1 for details). Cells were then incubated into a live cell imaging instrument (Incucyte®) for 6 to 8 days and their confluency was monitored all along the culture.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	WiDr cells		CVCL_2760

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	9- 4.6 × 10 -4 ug/mL	Positive ASCT2 expression (ASCT2+++/++)
Method Description	Target cells were seeded in triplicates into flat-bottom 384-wells plate (400 cells for HCT116 cells). Cells were incubated for 3 to 4 hours at 37°C before addition of an equivalent volume of 2X concentrated ADC or free drug-linker dose range (see table 1 for details). Cells were then incubated into a live cell imaging instrument (Incucyte®) for 6 to 8 days and their confluency was monitored all along the culture.    Click to Show/Hide
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	9- 4.6 × 10 -4 ug/mL	Positive ASCT2 expression (ASCT2+++/++)
Method Description	Target cells were seeded in triplicates into flat-bottom 384-wells plate (400 cells for HCT116 cells). Cells were incubated for 3 to 4 hours at 37°C before addition of an equivalent volume of 2X concentrated ADC or free drug-linker dose range (see table 1 for details). Cells were then incubated into a live cell imaging instrument (Incucyte®) for 6 to 8 days and their confluency was monitored all along the culture.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	WiDr cells		CVCL_2760

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.022 nM	High B7H3 expression (B7H3 +++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.034 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.201 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Negative B7H3 expression (B7H3-)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.048 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					[22]
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					[23]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.048 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					[23]
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					[22]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.08 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					[22]
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					[23]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.08 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					[23]
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					[24]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.22 nM	Positive CEA expression (CEA+++/++)
Method Description	NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.46 nM	Positive CEA expression (CEA+++/++)
Method Description	MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.12 nM	Positive CEA expression (CEA+++/++)
Method Description	Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Colon adenocarcinoma	Ls147T cells		CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Negative CEA expression (CEA-)
Method Description	MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	64 nM
Method Description	Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	100 nM
Method Description	Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561
Experiment 3 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	100 nM
Method Description	Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	66 nM
Method Description	Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	96 nM
Method Description	Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	100 nM
Method Description	Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	72 nM
Method Description	Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	96 nM
Method Description	Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	100 nM
Method Description	Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	72 nM
Method Description	Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	94 nM
Method Description	Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	100 nM
Method Description	Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	73 nM
Method Description	Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	95 nM
Method Description	Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Effective Concentration (EC50)	100 nM
Method Description	Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Half Maximal Effective Concentration (EC50)	285.967 nM	Positive HER expression (HER+++/++)
Method Description	In vitro cytotoxicity of the ADCs, isotype control ADCs, and reference free payloads were evaluated using the CellTiter-Glo 2.5 Assay Kit
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ -10%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line HS746T cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 5 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Gastric adenocarcinoma	HS746T cells		CVCL_0333
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ -5%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line BxPC3 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 10 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ -5%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line Calu6 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 10 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 0%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line NCI-H661 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 5 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Lung large cell carcinoma	NCI-H661 cells		CVCL_1577
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 5%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line U87.MG cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 5 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Glioblastoma	U87 MG cells		CVCL_0022
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 7%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line BxPC3 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 20 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC3 cells		CVCL_0186
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 8%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line T47D cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 5 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 10%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line NCI-H661 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 10 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Lung large cell carcinoma	NCI-H661 cells		CVCL_1577
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 15%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line HS746T cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 10 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Gastric adenocarcinoma	HS746T cells		CVCL_0333
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 15%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line U87.MG cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 10 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Glioblastoma	U87 MG cells		CVCL_0022
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 18%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line T47D cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 10 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 18%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line Calu6 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 20 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 20%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line NCI-H661 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 20 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Lung large cell carcinoma	NCI-H661 cells		CVCL_1577
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 25%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line BxPC3 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 40 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC3 cells		CVCL_0186
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 28%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line T47D cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 20 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 30%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line HS746T cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 20 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Gastric adenocarcinoma	HS746T cells		CVCL_0333
Experiment 17 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 35%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line U87.MG cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 20 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Glioblastoma	U87 MG cells		CVCL_0022
Experiment 18 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 38%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line T47D cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 40 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553
Experiment 19 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 38%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line Calu6 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 40 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 20 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 45%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line HS746T cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 40 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Gastric adenocarcinoma	HS746T cells		CVCL_0333
Experiment 21 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 60%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line NCI-H661 cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 40 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Lung large cell carcinoma	NCI-H661 cells		CVCL_1577
Experiment 22 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Cell growth inhibition ratio	≈ 75%	Positive CD47/PD-L1 expression (CD47/PD-L1+++/++)
Method Description	CD47/PD-L1-positive tumor cell line U87.MG cells were selected to be inoculated into 96-well plates with 3x105 cells/well and treated with the compound 93 with a dose of 40 ug/mL. Cell viability was measured by Cell Counting Kit-8 (CCK-8), and cell proliferation inhibition rate was calculated.
In Vitro Model	Glioblastoma	U87 MG cells		CVCL_0022

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