Linker ID	LIN0QDUUQ
Linker Name	N-succinimidyl 4-(2-pyridyldithio) pentanoate (SPP)
Linker Type	Thiol-sensitive linker
Antibody-Linker Relation	Cleavable
Structure
	3D MOL			2D MOL
Formula	C14H16N2O4S2
Isosmiles	CC(CCC(=O)ON1C(=O)CCC1=O)SSC2=CC=CC=N2
PubChem CID	11588139
InChI	InChI=1S/C14H16N2O4S2/c1-10(21-22-11-4-2-3-9-15-11)5-8-14(19)20-16-12(17)6-7-13(16)18/h2-4,9-10H,5-8H2,1H3
InChIKey	GTBCXYYVWHFQRS-UHFFFAOYSA-N
IUPAC Name	(2,5-dioxopyrrolidin-1-yl) 4-(pyridin-2-yldisulfanyl)pentanoate
Pharmaceutical Properties	Molecule Weight		340.4	Polar area		127
	Complexity		417	xlogp Value		1.5
	Heavy Count		22	Rot Bonds		8
	Hbond acc		7	Hbond Donor		0

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Objective Response Rate (ORR)	28.30%	Positive CD56 expression (CD56+++/++)
Patients Enrolled	Relapsed and/or Refractory CD-56-positive Multiple Myeloma.
Administration Dosage	40 mg/m2 (up to a maximum of 140 mg) intravenously once every 3 weeks.
Related Clinical Trial
NCT Number	NCT00346255	Clinical Status	Phase 1
Clinical Description	BB-10901 in treating patients with relapsed and/or refractory multiple myeloma (IMGN901).
Primary Endpoint	Objective response rate=28.30%.
Other Endpoint	Median progression-free survival=26.10 months (95% CI 1-89 weeks).

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.58% (Day 49)	Positive ITGAV expression (ITGAV +++/++)
Method Description	The rear flank region of female athymic rats were implanted with 5x106 cells subcutaneously (0.2 ml of25 x106 cells/ml) on the rear flank area. When mean tumor volumes reached to 250 mm3, dosed intravenously (15 mg/kg) on days 17 and 29 after tumor cell injection.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.88% (Day 37)	Positive ITGAV expression (ITGAV +++/++)
Method Description	Female athymic rats were inoculated with 5x106 HT29 cells subcutancously on the rear flank area. The animals were stratified into 13 groups, 6 animals per group based on a mean tumor volume for each group of approximately 250 mm3. On the day of grouping (day 7) each group received its initial dosing (175 ug/kg).
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.74% (Day 35)	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 3 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.54% (Day 35)	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 6 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.81% (Day 37)	Positive ITGAV expression (ITGAV +++/++)
Method Description	Female athymic rats were inoculated with 5x106 HT29 cells subcutancously on the rear flank area. The animals were stratified into 13 groups, 6 animals per group based on a mean tumor volume for each group of approximately 250 mm3. On the day of grouping (day 7) each group received its initial dosing (175 ug/kg).
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.21% (Day 24)	Positive ITGAV expression (ITGAV +++/++)
Method Description	Nine-week-old athymic nude rats were subcutaneously inoculated with A375.S2human melanoma cells. ADC (5 mg/kg) andappropriate control compounds were intravenously injected (three injection every other day inthe first week followed by one injection per week for two weeks.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 5 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.15% (Day 24)	Positive ITGAV expression (ITGAV +++/++)
Method Description	Nine-week-old athymic nude rats were subcutaneously inoculated with A375.S2human melanoma cells. ADC (10 mg/kg) andappropriate control compounds were intravenously injected (three injection every other day inthe first week followed by one injection per week for two weeks.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 6 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.23% (Day 35)	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 10 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 7 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.10% (Day 49)	Positive ITGAV expression (ITGAV +++/++)
Method Description	The rear flank region of female athymic rats were implanted with 5x106 cells subcutaneously (0.2 ml of25 x106 cells/ml) on the rear flank area. When mean tumor volumes reached to 250 mm3, dosed intravenously (15 mg/kg) on days 17 and 29 after tumor cell injection.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 8 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.81% (Day 35)	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 15 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.00 ug/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.20 ug/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.27 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 5 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.27 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Ovarian endometrioid adenocarcinoma	A2780 cells		CVCL_0134

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	32.17% (Day 30)	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Animals with established tumors of about 130 mm3 were treated with intravenous single injection of the M9346A-DM conjugates at 2.5±0.2 mg/kg, equivalent to 51±3 ug conjugated maytansinoid per kg The conjugates were injected on day 20 after cell inoculation.
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	50.00% (Day 32)	High FOLR1 expression (FOLR1+++; 1,300,000 FOLR1 molecules/cell)
Method Description	Animals with established tumors of about 130 mm3 were treated with intravenous single injection of the M9346A-DM conjugates at 2.5±0.2 mg/kg, equivalent to 51±3 ug conjugated maytansinoid per kg The conjugates were injected on day 7 after cell inoculation.
In Vivo Model	Ovarian carcinoma Igrov-1 CDX model
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11±0.04 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13±0.08 nM	Moderate FOLR1 expression (FOLR1++; 290,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363
Experiment 3 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14±0.05 nM	High FOLR1 expression (FOLR1+++; 1,300,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.55% (Day 27)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.55% (Day 27)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.32% (Day 27)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.00% (Day 9)	Positive CD19 expression (CD19+++/++)
Method Description	Animals with established subcutaneous xenograft Ramos tumors were treated with either huB4-SPP-DC4 (DC4 dose of 75 ug/kg, qdx5), or huB4-SPP-DC44 (DC44 dose of 75 ug/kg, qdx5), unconjugated DC4 (75 ug/kg, qdx5), unconjugated DC44 (75 ug/kg, qdx5), or with phosphate-buffered saline vehicle (control), administered intravenously, and the tumor growth was monitored.    Click to Show/Hide
In Vivo Model	Ramos CDX model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive CD19 expression (CD19+++/++)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (with acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1.80 nM	Negative CD19 expression(CD19-)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (with acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.45% (Day 20)	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.60% (Day 10)	High HER2 expression (HER2+++)
Method Description	Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.    Click to Show/Hide
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 (IC50)	4.26 nM	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	41.37 nM	Negative HER2 expression (HER2-)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Low HER2 expression (HER2+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.61% (Day 30)	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.27% (Day 20)	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.11% (Day 30)	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 450 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM-10.00 nM	Positive CD138 expression (CD138 +++/++)
Method Description	CD138+ MOLP-8 cells were seeded in flat bottom plates at 3000 cells/well. CD138- BJAB control cells were seeded at 1000 cells/weli. The cells were treated with nBT062-SPDB-DM4nBT062-SPP-DM1 or nBT062-SMCC-DM1 at different concentrations for five days.
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD138 expression (CD138 -)
Method Description	CD138+ MOLP-8 cells were seeded in flat bottom plates at 3000 cells/well. CD138- BJAB control cells were seeded at 1000 cells/weli. The cells were treated with nBT062-SPDB-DM4nBT062-SPP-DM1 or nBT062-SMCC-DM1 at different concentrations for five days.
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.00% (Day 9)	Positive CD19 expression (CD19+++/++)
Method Description	Animals with established subcutaneous xenograft Ramos tumors were treated with either huB4-SPP-DC4 (DC4 dose of 75 ug/kg, qdx5), or huB4-SPP-DC44 (DC44 dose of 75 ug/kg, qdx5), unconjugated DC4 (75 ug/kg, qdx5), unconjugated DC44 (75 ug/kg, qdx5), or with phosphate-buffered saline vehicle (control), administered intravenously, and the tumor growth was monitored.    Click to Show/Hide
In Vivo Model	Ramos CDX model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 pM	Positive CD19 expression (CD19+++/++)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (without acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.74 nM	Positive CD19 expression (CD19+++/++)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (with acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1.50 nM	Negative CD19 expression(CD19-)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (with acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 4 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3.00 nM	Negative CD19 expression(CD19-)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (without acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.72% (Day 17)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	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					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.09% (Day 17)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	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 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 3 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing 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 4 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 5 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	Moderate FOLR1 expression (FOLR1 ++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.98% (Day 20)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of OVCAR-3 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.50% (Day 30)	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established in SCID mice.A subcutaneous model of the human pancreatic cancer cell-line HPAC was developed. The dose was 27.7 mg/kg qw x2.
In Vivo Model	HPAC CDX model
In Vitro Model	Pancreatic adenocarcinoma	HPAC cells		CVCL_3517
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 30)	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established in SCID mice.A subcutaneous model of the human cervical cancer cell-line HeLa was developed. The dose was 27.7 mg/kg qw x2.
In Vivo Model	HeLa CDX model
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 30)	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established in SCID mice.A subcutaneous model of the human ovarian cancer cell-line TOV-21G was developed. The dose was 27.7 mg/kg qw x2.
In Vivo Model	TOV-21G CDX model
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 30)	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established inSCID mice.A subcutaneous model of the human cervicalcarcinoma cell-line KB was developed. The dose was 150 ug/kg every day for 5 days.
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					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 30)	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established inSCID mice.A subcutaneous model of the human cervicalcarcinoma cell-line KB was developed. The dose was 250 ug/kg every day for 5 days.
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					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 30)	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established inSCID mice.A subcutaneous model of the human cervicalcarcinoma cell-line KB was developed. The dose was 27.7 mg/kg qw x2.
In Vivo Model	OVCAR-5 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-5 cells		CVCL_1628

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Ductal carcinoma	BT-483 cells		CVCL_2319
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.45 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.46 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	WISH cells		CVCL_1909
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.67 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Endocervical adenocarcinoma	WISH cells		CVCL_1909
Experiment 5 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.80 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	Caov-3 cells		CVCL_0201
Experiment 6 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.40 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 7 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.61 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Ovarian serous adenocarcinoma	Caov-3 cells		CVCL_0201
Experiment 8 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.80 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 9 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.80 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Pancreatic adenocarcinoma	HPAC cells		CVCL_3517
Experiment 10 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.84 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Pancreatic adenocarcinoma	HPAC cells		CVCL_3517
Experiment 11 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613
Experiment 12 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 13 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	High grade ovarian serous adenocarcinoma	Caov-4 cells		CVCL_0202
Experiment 14 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 15 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Pancreatic adenocarcinoma	Hs 766T cells		CVCL_0334
Experiment 16 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-5 cells		CVCL_1628
Experiment 17 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 18 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588
Experiment 19 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.01 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 20 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.88 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613
Experiment 21 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 22 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.40 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 23 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Ductal carcinoma	BT-483 cells		CVCL_2319
Experiment 24 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	High grade ovarian serous adenocarcinoma	Caov-4 cells		CVCL_0202
Experiment 25 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 26 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 27 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.00 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Pancreatic adenocarcinoma	Hs 766T cells		CVCL_0334
Experiment 28 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	846 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-5 cells		CVCL_1628

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.40 pM	Positive CD19 expression (CD19+++/++)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (without acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.30 nM	Negative CD19 expression(CD19-)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (without acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.00 ug/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.50 ug/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.29 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.30 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Ovarian endometrioid adenocarcinoma	A2780 cells		CVCL_0134
Experiment 5 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.42 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Objective Response Rate (ORR)	0.00%
Patients Enrolled	Metastatic breast cancer (MBC) that expresses CD44v6 in at least 50% of tumor cells in primary tumor tissue as assessed by immunohistochemistry, pretreatment with anthracyclines and taxanes, tumor metastases measurable by computed tomography (CT) or magnetic resonance imaging (MRI), life expectancy of at least 6 months, no chemotherapy, radiotherapy or immunotherapy within the last 4 weeks before study entry, adequate organ function, Eastern Cooperative Oncology Group performance score 2.    Click to Show/Hide
Administration Dosage	One single intravenous infusion over 30 min, dose was escalated in 25 mg/m2 increments up to the maximum tolerated dose (MTD).
Related Clinical Trial
NCT Number	NCT02254005	Clinical Status	Phase 1
Clinical Description	An open phase 1 single dose escalation study of bivatuzumab mertansine administered intravenously in female patients with CD44v6 positive metastatic breast cancer with repeated administration in patients with clinical benefit.
Primary Endpoint	The MTD in this trial could not be determined.
Other Endpoint	No objective responses were observed. Disease stabilization was achieved in 50.00% of patients independently of dose level.
Experiment 2 Reporting the Activity Date of This ADC					[12]
Related Clinical Trial
NCT Number	NCT02254044	Clinical Status	Phase 1
Clinical Description	An open phase 1 dose escalation study of bivatuzumab mertansine administered intravenously once per week for three weeks in patients with advanced squamous cell carcinoma of the head and neck or esophagus with repeated administration courses in patients with clinical benefit.
Experiment 3 Reporting the Activity Date of This ADC					[13]
Patients Enrolled	Ecurrent or metastatic head and neck squamous cell carcinoma (HNSCC) not amenable to established treatments, an ECOG score 2, and an estimated life expectancy of at least 6 months, a tumor diameter of at least 1 cm in CT or MRI scans was also required.
Administration Dosage	Starting with 25 mg/m2, the dose was escalated in steps of 25 mg/m2 until dose limiting toxicity was observed, intravenously.
Related Clinical Trial
NCT Number	NCT02254044	Clinical Status	Phase 1
Clinical Description	An open phase 1 dose escalation study of bivatuzumab mertansine administered intravenously once per week for three weeks in patients with advanced squamous cell carcinoma of the head and neck or esophagus with repeated administration courses in patients with clinical benefit.
Primary Endpoint	The MTD was 300 mg/m2.
Other Endpoint	Due to the premature discontinuation of the trial efficacy complying with the study plan could not be assessed. In 3 patients,a partial response at doses of 2.00, 2.75 and 3.25 mg/m2.
Experiment 4 Reporting the Activity Date of This ADC					[14]
Related Clinical Trial
NCT Number	NCT02254031	Clinical Status	Phase 1
Clinical Description	An open phase 1 dose escalation study of bivatuzumab mertansine administered intravenously once per week for three weeks in female patients with CD44V6 positive recurrent or metastatic breast cancer with repeated administration courses in patients with clinical.
Experiment 5 Reporting the Activity Date of This ADC					[15]
Related Clinical Trial
NCT Number	NCT02254018	Clinical Status	Phase 1
Clinical Description	An open phase 1 single dose escalation study of bivatuzumab mertansine administered intravenously in patients with advanced squamous cell carcinoma of the head and neck with repeated administration in patients with clinical benefit.
Experiment 6 Reporting the Activity Date of This ADC					[16]
Related Clinical Trial
NCT Number	NCT02254005	Clinical Status	Phase 1
Clinical Description	An open phase 1 single dose escalation study of bivatuzumab mertansine administered intravenously in female patients with CD44v6 positive metastatic breast cancer with repeated administration in patients with clinical benefit.

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Objective Response Rate (ORR)	0.00%
Patients Enrolled	Histological documentation of advanced or metastatic epithelial solid tumor which were likely to express the CanAg antigen, that were refractory or resistant to standard chemotherapy, or for which no effective standard therapy exists.
Administration Dosage	IV infusion at an initial dose of 30 mg/m2, three times per week for three consecutive weeks for a total of nine doses.
Experiment 2 Reporting the Activity Date of This ADC					[17]
Patients Enrolled	Solid malignancies refractory to standard therapy or for whom no standard therapy existed.
Administration Dosage	IV cantuzumab mertansine was administered at a rate of 1 mg/min for 30 minutes and then increased to 3 mg/min if hypersensitivity phenomena were not observed. Treatment courses were repeated every 3 weeks.

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