Antibody Information

General Information of This Antibody

Antibody ID	ANI0UMBRJ
Antibody Name	Anti-NOTCH3 mAb hu28
Antibody Type	Monoclonal antibody (mAb)
Antibody Subtype	Humanized IgG1-kappa
Antigen Name	Neurogenic locus notch homolog protein 3 (NOTCH3)	Antigen Info

Each Antibody-drug Conjugate Related to This Antibody

Full Information of The Activity Data of The ADC(s) Related to This Antibody

hu28-vc6780 [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.20% (Day 63)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 10 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	Non small cell lung cancer PDX model (PDX: 37622A1)

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 9 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 23.90% (Day 19)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 29.60% (Day 10)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	HCC2429 CDX model
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 29.60% (Day 33)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 38.00% (Day 19)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.90% (Day 33)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.70% (Day 10)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	HCC2429 CDX model
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 7 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.80% (Day 33)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 10 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 8 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.80% (Day 19)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 10 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 9 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.00% (Day 10)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 10 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	HCC2429 CDX model
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132

Revealed Based on the Cell Line Data

Click To Hide/Show 6 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.30 ng/mL	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
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 Inhibitory Concentration (IC50)	17.00 ng/mL	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	148.00 ng/mL	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.15 nM	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.24 nM	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Osteosarcoma	U2OS cells		CVCL_0042
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.24 nM	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

hu28-vc0101 [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.60% (Day 63)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	Non small cell lung cancer PDX model (PDX: 37622A1)

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 14 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 18.30% (Day 13)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	HCC2429 CDX model
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.40% (Day 49)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.00% (Day 26)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.30% (Day 50)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.90% (Day 13)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	HCC2429 CDX model
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.50% (Day 49)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 7 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.40% (Day 47)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 8 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.20% (Day 13)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	HCC2429 CDX model
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 9 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.70% (Day 33)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 10 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.80% (Day 33)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 11 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.50% (Day 50)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 12 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.10% (Day 33)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 13 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.20% (Day 49)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 14 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg, Q4d*4 to thetail of each mouse.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Revealed Based on the Cell Line Data

Click To Hide/Show 8 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.20 ng/mL	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
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 Inhibitory Concentration (IC50)	306.00 ng/mL	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	473.00 ng/mL	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.33 ug/mL	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Osteosarcoma	U2OS cells		CVCL_0042
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ug/mL	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.18 nM	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Lung non-small cell carcinoma	HCC2429 cells		CVCL_5132
Experiment 7 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.27 nM	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Osteosarcoma	U2OS cells		CVCL_0042
Experiment 8 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.27 nM	Positive NOTCH3 expression (NOTCH3+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO₂ before assaying. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

PF-06650808 [Terminated in phase 1]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Objective Response Rate (ORR)	9.68% (all response-evaluable patients) 16.67% (patients with breast cancer) 21.43% (patients with ER+ breast cancer)
Patients Enrolled	Locally advanced/metastatic solid tumors resistant to standard therapy or with no available standard therapy; Eastern Cooperative Oncology Group (ECOG) performance score (PS) 01; a life expectancy 12 weeks; and adequate bone marrow, hepatic, and renal function.
Administration Dosage	Intravenously every 3 weeks (Q3W) starting at a dose of 0.20 mg/kg to be escalated up to 6.40 mg/kg, following the modified continual reassessment method (mCRM).
*Related Clinical Trial*
NCT Number	NCT02129205	Clinical Status	Phase 1
Clinical Description	A phase 1 dose escalation study evaluating the safety and tolerability of PF-06650808 In patients with advanced solid tumors.
Primary Endpoint	OrR=9.68% for all response-evaluable patients (N=3/31), ORR=16.67% for patients with breast cancer (N=3/18), ORR=21.43% for patients with ER+ breast cancer (N=3/14). Five patients with advanced BC achieved PR as best overall response (BOR): 2 at 2.0 mg/kg, 1 at 2.4 mg/kg, and 2 at 3.6 mg/kg.
Other Endpoint	The maximum tolerated dose (MTD) was estimated to be 2.40 mg/kg.
Experiment 2 Reporting the Activity Date of This ADC				[3]
*Related Clinical Trial*
NCT Number	NCT02129205	Clinical Status	Phase 1
Clinical Description	A phase 1 dose escalation study evaluating the safety and tolerability of PF-06650808 in patients with advanced solid tumors.

References

Ref 1	Anti-notch3 antibodies and antibody-drug conjugates.
Ref 2	A phase I, dose-escalation study of PF-06650808, an anti-Notch3 antibody-drug conjugate, in patients with breast cancer and other advanced solid tumors. Invest New Drugs. 2020 Feb;38(1):120-130.
Ref 3	A PHASE 1 DOSE ESCALATION STUDY EVALUATING THE SAFETY AND TOLERABILITY OF PF-06650808 IN PATIENTS WITH ADVANCED SOLID TUMORS

Antibody Information

Citation

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Correspondence

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)