Linker ID	LIN0TUWCX
Linker Name	CB07 linker
Linker Type	Unclear
Antibody-Linker Relation	Unclear
Structure
	3D MOL			2D MOL
Formula	C46H74N8O17
Isosmiles	CC(C)[C@H](NC([C@@H](NC(CN1C(C=CC1=O)=O)=O)CCNC(CCOCCOCCOCCOCCOCCOCCOCCOC)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC2=CC=C(CO)C=C2)=O)=O
InChI	InChI=1S/C46H74N8O17/c1-33(2)42(45(62)52-36(5-4-14-49-46(47)63)43(60)50-35-8-6-34(32-55)7-9-35)53-44(61)37(51-39(57)31-54-40(58)10-11-41(54)59)12-15-48-38(56)13-16-65-19-20-67-23-24-69-27-28-71-30-29-70-26-25-68-22-21-66-18-17-64-3/h6-11,33,36-37,42,55H,4-5,12-32H2,1-3H3,(H,48,56)(H,50,60)(H,51,57)(H,52,62)(H,53,61)(H3,47,49,63)/t36-,37-,42-/m0/s1
InChIKey	GWHVMLYGDAXNDO-LIGBGABDSA-N
Pharmaceutical Properties	Molecule Weight		1011.137	Polar area		332.07
	Complexity		1681.541003	xlogp Value		-1.7397
	Heavy Count		71	Rot Bonds		42
	Hbond acc		17	Hbond Donor		8

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	71.59%	Positive FR-alpha expression (FR-alpha+++/++)
Method Description	In the OV3756 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	OV3756 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	71.59%	Positive FR-alpha expression (FR-alpha+++/++)
Method Description	In the OV3756 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	OV3756 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	86.48%	Positive Trop2 expression (Trop2+++/++)
Method Description	In the MX-1 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
In Vivo Model	MX-1 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	86.48%	Positive Trop2 expression (Trop2+++/++)
Method Description	In the MX-1 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
In Vivo Model	MX-1 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	109.48%	Positive Trop2 expression (Trop2+++/++)
Method Description	In the MX-1 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	MX-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	109.48%	Positive Trop2 expression (Trop2+++/++)
Method Description	In the MX-1 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	MX-1 xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	114.40%	Positive Trop2 expression (Trop2+++/++)
Method Description	In the Capan-1 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	Capan-1 xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	114.40%	Positive Trop2 expression (Trop2+++/++)
Method Description	In the Capan-1 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	Capan-1 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	157.8 ng/mL	Positive Trop2 expression (Trop2+++/++)
Method Description	MDA-MB-468 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC4 for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	233 ng/mL	Positive Trop2 expression (Trop2+++/++)
Method Description	MX-1 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC4 for 120 h.
In Vitro Model	Breast carcinoma	MX-1 cells		CVCL_4774
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	640 ng/mL	Positive Trop2 expression (Trop2+++/++)
Method Description	MDA-MB-453 were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC4 for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 15000 ng/mL	Negative Trop2 expression (Trop2-)
Method Description	HGC27 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC4 for 120 h.
In Vitro Model	Gastric carcinoma	HGC27 cells		CVCL_1279

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	86.81%	Positive FR-alpha expression (FR-alpha+++/++)
Method Description	In the OV3756 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
In Vivo Model	OV3756 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	86.81%	Positive FR-alpha expression (FR-alpha+++/++)
Method Description	In the OV3756 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
In Vivo Model	OV3756 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.645 nM	Positive FR-alpha expression (FR-alpha+++/++)
Method Description	MCF-7 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC16 (4x the first top concentration at 250 nM) for 5 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.645 nM	Positive FR-alpha expression (FR-alpha+++/++)
Method Description	MCF-7 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC16 (4x the first top concentration at 250 nM) for 5 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.611 nM	Positive FR-alpha expression (FR-alpha+++/++)
Method Description	JEG-3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC16 (4x the first top concentration at 1000 nM) for 5 days.
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.611 nM	Positive FR-alpha expression (FR-alpha+++/++)
Method Description	JEG-3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC16 (4x the first top concentration at 1000 nM) for 5 days.
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	93.86%	Positive B7H3 expression (B7H3+++/++)
Method Description	In the Hep-3 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
In Vivo Model	Hep-3 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	93.86%	Positive B7H3 expression (B7H3+++/++)
Method Description	In the Hep-3 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
In Vivo Model	Hep-3 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.66%	Positive B7H3 expression (B7H3+++/++)
Method Description	In the Hep-3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	Hep-3 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.66%	Positive B7H3 expression (B7H3+++/++)
Method Description	In the Hep-3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	Hep-3 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. nM	Negative B7H3 expression (B7H3-)
Method Description	5000 CHO-K1 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
In Vitro Model	Normal	CHO-K1 cells		CVCL_0214
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.35 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	5000 CHO-K1-B7-H3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
In Vitro Model	Normal	CHO-K1-B7-H3 cells		CVCL_0214
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.35 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	5000 CHO-K1-B7-H3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
In Vitro Model	Normal	CHO-K1-B7-H3 cells		CVCL_0214
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	16.32 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	5000 Calu-6 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	16.32 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	5000 Calu-6 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.53%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.53%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	105.80%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	105.80%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	36 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	MDA-MB-453 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	43 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	62 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	BT-474 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	82 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10000 ng/mL	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Ref 1	Drug conjugates and uses thereof