Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0GMTZZ
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| ADC Name |
hu75-vc0101
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| Synonyms |
hu75 vc0101
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| Organization |
Pfizer Inc.
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| Drug Status |
Investigative
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| Indication |
In total 4 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Non small cell lung cancer [ICD11:2C25]
Investigative
Osteosarcoma [ICD11:2B51]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
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| Drug-to-Antibody Ratio |
3.8
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| Antibody Name |
Anti-NOTCH3 mAb hu75
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Antibody Info | ||||
| Antigen Name |
Neurogenic locus notch homolog protein 3 (NOTCH3)
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Antigen Info | ||||
| Payload Name |
Undisclosed
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| Linker Name |
hu75-vc0101 linker
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General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
| Standard Type | Value | Units | Animal Model (No. of PDX) |
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| Tumor Growth Inhibition value (TGI) |
≈ 52.5
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%
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Non small cell lung cancer PDX model (PDX: 37622A1)
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Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 52.50% (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.
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| In Vivo Model | Non small cell lung cancer PDX model (PDX: 37622A1) | ||||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 3.80% (Day 42) | 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.
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| 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) | ≈ 25.60% (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.
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| 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) | ≈ 44.30% (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 1 mg/kg, Q4d*4 to thetail of each mouse.
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| In Vivo Model | HCC2429 CDX model | ||||
| In Vitro Model | Lung non-small cell carcinoma | HCC2429 cells | CVCL_5132 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 62.30% (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.
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| 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) | ≈ 83.00% (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.
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| 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) | ≈ 91.60% (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.
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| 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) | ≈ 93.80% (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.
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| 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) | ≈ 95.10% (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.
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| In Vivo Model | NCI-N87 CDX model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 35) | 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.
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| 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
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 37.00 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.
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| 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) | 515.00 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.
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| 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) | 523.00 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.
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| In Vitro Model | Osteosarcoma | U2OS cells | CVCL_0042 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 611.00 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.
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| 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) | 0.43 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.
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| In Vitro Model | Lung non-small cell carcinoma | HCC2429 cells | CVCL_5132 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.80 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
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| In Vitro Model | Osteosarcoma | U2OS cells | CVCL_0042 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 2.02 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.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
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