Payload ID	PAY0BVTPA
Name	Tetrahydroisoquinoline-based PBD dimer 17
Synonyms	Tetrahydroisoquinoline-based PBD dimer 17    Click to Show/Hide
Target(s)	Human Deoxyribonucleic acid (hDNA)					Target Info

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.80%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.005 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.48%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.02 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.07%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.01 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.03 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.06 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.24%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.005 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.58%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.02 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.20 nM	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MSLN expression (MSLN+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative MSLN expression (MSLN-)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MSLN expression (MSLN+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive MSLN expression (MSLN+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.00 nM	Negative MSLN expression (MSLN-)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive MSLN expression (MSLN+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	37.80 nM	Negative MSLN expression (MSLN-)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.90 nM	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.50 nM	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.60 nM	Negative CD70 expression (CD70-)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Ref 1	Design, Synthesis, and Structure-Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody-Drug Conjugates. J Med Chem. 2020 Nov 25;63(22):13913-13950. doi: 10.1021/acs.jmedchem.0c01385.