Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0NTWRT
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| ADC Name |
Fab-SN38
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| Synonyms |
Fab-SN38; Anti-HER2 Fab-SN38 conjugate
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| Organization |
School of Pharmaceutical Sciences, Wuhan University.
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| Drug Status |
Investigative
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| Structure |
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| Antibody Name |
Anti-HER2 Fab
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
Active metabolite of irinotecan SN38
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
LPETGGG-PEG3-Azide BCN-AVC
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Linker Info | ||||
| Conjugate Type |
Site-specific bioconjugation via sortase A.
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General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 2.23۪.14 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
The cytotoxicity of Fab-SN38 was evaluated using the Cell Counting Kit-8 (CCK-8) assay. Cells (MDA-MB-231, Calu-3, NCI-N87 and SK-OV-3 cells) were seeded into clear-bottom 96-well plates (~3000 cells per well). After overnight culture, the medium was removed and the fresh medium containing SN38, Glu (SN38)-OH, Glu-SN38, trastuzumab, the Fab protein or the Fab-SN38 conjugate was added and incubated for 72 h at 37 °C in a CO2 incubator. Cell viability was measured using the CCK-8 reagent according to the protocol. Briefly, 15 uL of CCK-8 solution was added to the culture media. Two hours after incubation at 37 °C, the absorbance at a wavelength of 450 nm was measured by a microplate reader (TECAN, Switzerland) and then the IC50 value was profiled using the Graphpad Prism 8 software.
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| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 3.5۪.16 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
The cytotoxicity of Fab-SN38 was evaluated using the Cell Counting Kit-8 (CCK-8) assay. Cells (MDA-MB-231, Calu-3, NCI-N87 and SK-OV-3 cells) were seeded into clear-bottom 96-well plates (~3000 cells per well). After overnight culture, the medium was removed and the fresh medium containing SN38, Glu (SN38)-OH, Glu-SN38, trastuzumab, the Fab protein or the Fab-SN38 conjugate was added and incubated for 72 h at 37 °C in a CO2 incubator. Cell viability was measured using the CCK-8 reagent according to the protocol. Briefly, 15 uL of CCK-8 solution was added to the culture media. Two hours after incubation at 37 °C, the absorbance at a wavelength of 450 nm was measured by a microplate reader (TECAN, Switzerland) and then the IC50 value was profiled using the Graphpad Prism 8 software.
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| In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 8.47۪.29 nM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
The cytotoxicity of Fab-SN38 was evaluated using the Cell Counting Kit-8 (CCK-8) assay. Cells (MDA-MB-231, Calu-3, NCI-N87 and SK-OV-3 cells) were seeded into clear-bottom 96-well plates (~3000 cells per well). After overnight culture, the medium was removed and the fresh medium containing SN38, Glu (SN38)-OH, Glu-SN38, trastuzumab, the Fab protein or the Fab-SN38 conjugate was added and incubated for 72 h at 37 °C in a CO2 incubator. Cell viability was measured using the CCK-8 reagent according to the protocol. Briefly, 15 uL of CCK-8 solution was added to the culture media. Two hours after incubation at 37 °C, the absorbance at a wavelength of 450 nm was measured by a microplate reader (TECAN, Switzerland) and then the IC50 value was profiled using the Graphpad Prism 8 software.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
The cytotoxicity of Fab-SN38 was evaluated using the Cell Counting Kit-8 (CCK-8) assay. Cells (MDA-MB-231, Calu-3, NCI-N87 and SK-OV-3 cells) were seeded into clear-bottom 96-well plates (~3000 cells per well). After overnight culture, the medium was removed and the fresh medium containing SN38, Glu (SN38)-OH, Glu-SN38, trastuzumab, the Fab protein or the Fab-SN38 conjugate was added and incubated for 72 h at 37 °C in a CO2 incubator. Cell viability was measured using the CCK-8 reagent according to the protocol. Briefly, 15 uL of CCK-8 solution was added to the culture media. Two hours after incubation at 37 °C, the absorbance at a wavelength of 450 nm was measured by a microplate reader (TECAN, Switzerland) and then the IC50 value was profiled using the Graphpad Prism 8 software.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||