Linker ID	LIN0XOHOG
Linker Name	OXDc-VA-PAB (PEG)
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
	3D MOL			2D MOL
Formula	C81H137N9O33S
Isosmiles	COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCN1C=C(N=N1)CC(O)C2=CC=C(NC([C@@H](NC([C@@H](NC(COCC(NCC3=CC=CC(C4=NN=C(O4)S(C)(=O)=O)=C3)=O)=O)C(C)C)=O)C)=O)C=C2
InChI	InChI=1S/C81H137N9O33S/c1-67(2)77(85-76(93)66-122-65-75(92)82-63-69-7-6-8-71(61-69)80-87-88-81(123-80)124(5,96)97)79(95)83-68(3)78(94)84-72-11-9-70(10-12-72)74(91)62-73-64-90(89-86-73)13-14-99-17-18-101-21-22-103-25-26-105-29-30-107-33-34-109-37-38-111-41-42-113-45-46-115-49-50-117-53-54-119-57-58-121-60-59-120-56-55-118-52-51-116-48-47-114-44-43-112-40-39-110-36-35-108-32-31-106-28-27-104-24-23-102-20-19-100-16-15-98-4/h6-12,61,64,67-68,74,77,91H,13-60,62-63,65-66H2,1-5H3,(H,82,92)(H,83,95)(H,84,94)(H,85,93)/t68-,74?,77-/m0/s1
InChIKey	RMDXCIULCVMJEA-FWAGEXBNSA-N
Pharmaceutical Properties	Molecule Weight		1797.084	Polar area		471.15
	Complexity		.	xlogp Value		0.9529
	Heavy Count		124	Rot Bonds		89
	Hbond acc		38	Hbond Donor		5

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	63%	High CD123 expression (CD123+++)
Method Description	Investigated the antitumour effect of 5mg/kg ADC in a CD33highCD123high MV-4-11 xenograft NOD SCID mice tumour model, D19.
In Vivo Model	CD123-high MV-4-11 xenograft NOD SCID mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2666 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	65%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 3mg/kg T-ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D26.
In Vivo Model	HER2-low JIMT-1 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.60%	High HER2 expression (HER2+++)
Method Description	Investigated the antitumour effect of 3mg/kg ADC in a HER2high HCC-1954 xenograft NUNU mice tumour model, D21.
In Vivo Model	HER2-high HCC-1954 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	88%	High HER2 expression (HER2+++)
Method Description	Investigated the antitumour effect of 3mg/kg ADC in a HER2high HCC-1954 xenograft NUNU mice tumour model, D21.
In Vivo Model	HER2-high HCC-1954 xenograft NUNU mice tumour model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 5mg/kg ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D13.
In Vivo Model	HER2-low JIMT-1 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.8 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to BT-474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
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 inhibitory Concentration (lC50)	0.01676 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of ADC to T-47D cells
In Vitro Model	Invasive breast carcinoma of no special type	T-47D cells		CVCL_0553
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.4645 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100.20%	High CD33 expression (CD33+++)
Method Description	Investigated the antitumour effect of 0.1 mg/kg ADC in a CD33highCD123high MV-4-11 xenograft NOD SCID mice tumour model, D14.
In Vivo Model	CD123-high MV-4-11 xenograft NOD SCID mice tumour model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	108.60%	High CD33 expression (CD33+++)
Method Description	Investigated the antitumour effect of 1mg/kg ADC in a CD33high MV-4-11 xenograft NOD SCID mice tumour model, D19.
In Vivo Model	CD33-high MV-4-11 xenograft NOD SCID mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.475 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	108.30%	High CD33 expression (CD33+++)
Method Description	Investigated the antitumour effect of 1mg/kg ADC in a CD33high MV-4-11 xenograft NOD SCID mice tumour model, D19.
In Vivo Model	CD33-high MV-4-11 xenograft NOD SCID mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.486 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	108.70%	High CD33 expression (CD33+++)
Method Description	Investigated the antitumour effect of 1mg/kg ADC in a CD33high MV-4-11 xenograft NOD SCID mice tumour model, D19.
In Vivo Model	CD33-high MV-4-11 xenograft NOD SCID mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.355 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.404 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.12 nM	High BCMA expression (BCMA+++)
Method Description	Cytotoxicity of ADC to NCI-H929 cells
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.21 nM	High BCMA expression (BCMA+++)
Method Description	Cytotoxicity of ADC to NCI-H929 cells
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Ref 1	Antibody-drug conjugate