Linker ID	LIN0GQTJP
Linker Name	PEG4-Mal
Linker Type	Flexible reactive (thiol) linker
Antibody-Linker Relation	Uncleavable
Structure
	3D MOL			2D MOL
Formula	C22H31N3O11
Isosmiles	O=C(CCN1C(=O)C=CC1=O)NCCOCCOCCOCCOCCC(=O)ON1C(=O)CCC1=O
InChI	InChI=1S/C22H31N3O11/c26-17(5-8-24-18(27)1-2-19(24)28)23-7-10-33-12-14-35-16-15-34-13-11-32-9-6-22(31)36-25-20(29)3-4-21(25)30/h1-2H,3-16H2,(H,23,26)
InChIKey	XSRYGQJQNPJNKZ-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight		513.5	Polar area		167.08
	Complexity		36	xlogp Value		-1.5186
	Heavy Count		36	Rot Bonds		19
	Hbond acc		11	Hbond Donor		1

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 18.22% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 3 post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	FOLR1-expressing SKOV3 cells were incubated with varying concentrations of anti FOLR1 antibodies or their conjugates and processed.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.03% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 3 post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	FOLR1-expressing SKOV3 cells were incubated with varying concentrations of anti FOLR1 antibodies or their conjugates and processed.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 24.92% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 2.5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.37% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 5 mg/kg ofone of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68.53% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 3 post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.02% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.21% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 10 mg/kg (every week, three weeks) of one of the conjugates listed above or with PBS only.    Click to Show/Hide
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 30)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Mice were randomized by body weight into treatment groups and reated either singly (SPDB conjugates) on day 3 post cell inoculation, or three times weekly on days 3, 10, and 17 post KB cell inoculation with 10 mg/kg of a conjugate.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	FOLR1-expressing SKOV3 cells were incubated with varying concentrations of anti FOLR1 antibodies or their conjugates and processed.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.33% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 3 post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	FOLR1-expressing SKOV3 cells were incubated with varying concentrations of anti FOLR1 antibodies or their conjugates and processed.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.84% (Day 22)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	PEG4Mal-DM4 conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 3 post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	FOLR1-expressing SKOV3 cells were incubated with varying concentrations of anti FOLR1 antibodies or their conjugates and processed.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	FOLR1-expressing SKOV3 cells were incubated with varying concentrations of anti FOLR1 antibodies or their conjugates and processed.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	FOLR1-expressing SKOV3 cells were incubated with varying concentrations of anti FOLR1 antibodies or their conjugates and processed.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	A PEG4-mal-DM4 conjugate in various concentrations was added to FOLR1-expressing KB cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	A PEG4-mal-DM4 conjugate in various concentrations was added to FOLR1-expressing KB cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM-10.00 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	A PEG4-mal-DM4 conjugate in various concentrations was added to FOLR1-expressing KB cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium. Antibodies and conjugates were diluted into complete RPMI medium using 3-fold dilution seriesand 100 pL were added per well.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM-10.00 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	A PEG4-mal-DM4 conjugate in various concentrations was added to FOLR1-expressing KB cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium. Antibodies and conjugates were diluted into complete RPMI medium using 3-fold dilution seriesand 100 pL were added per well.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Ref 1	Folate receptor 1 antibodies and immunoconjugates and uses thereof; 2011-09-01.