Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0YLEMF
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| ADC Name |
Hu001-3-MMAE
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| Synonyms |
Hu001-3-MMAE
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| Organization |
Hefei Institutes of Physical Science
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
4.15
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| Structure |
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| Antibody Name |
Hu001-3
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Antibody Info | ||||
| Antigen Name |
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Mc-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
Vedotin
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Tumor Growth lnhibition value (TGl) |
73.82
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%
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Undisclosed | Undisclosed |
| Tumor Growth lnhibition value (TGl) |
94.89
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%
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Undisclosed | Undisclosed |
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | 73.82% | High ROR1 expression (ROR1 +++) | ||
| Method Description |
Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, QwƧ) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
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| In Vivo Model | MDA-MB-231 xenograft model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | 94.89% | High ROR1 expression (ROR1 +++) | ||
| Method Description |
Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, QwƧ) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
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| In Vivo Model | MDA-MB-231 xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 4.13 nM | High ROR1 expression (ROR1 +++) | ||
| Method Description |
A total of 250-1500cells (PA-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Ovarian mixed germ cell tumor | PA-1 cells | CVCL_0479 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 4.15 nM | High ROR1 expression (ROR1 +++) | ||
| Method Description |
A total of 250-1500cells (NCI-H446) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Lung small cell carcinoma | NCI-H446 cells | CVCL_1562 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 4.18 nM | High ROR1 expression (ROR1 +++) | ||
| Method Description |
A total of 250-1500cells (HCC1187) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Breast ductal carcinoma | HCC1187 cells | CVCL_1247 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 6.25 nM | High ROR1 expression (ROR1 +++) | ||
| Method Description |
A total of 250-1500cells (NCI-N87) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 9.6 nM | High ROR1 expression (ROR1 +++) | ||
| Method Description |
A total of 250-1500cells (SK-CO-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Colon adenocarcinoma | SKCO1 cells | CVCL_0626 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 14.72 nM | Moderate ROR1 expression (ROR1++) | ||
| Method Description |
A total of 250-1500cells (COLO-678) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Colon carcinoma | COLO-678 cells | CVCL_1129 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 15.79 nM | High ROR1 expression (ROR1 +++) | ||
| Method Description |
A total of 250-1500cells (MDA-MB-231) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 17.78 nM | High ROR1 expression (ROR1 +++) | ||
| Method Description |
A total of 250-1500cells (HT-29) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Colon adenocarcinoma | HT-29 cells | CVCL_0320 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 26.67 nM | High ROR1 expression (ROR1 +++) | ||
| Method Description |
A total of 250-1500cells (HCC827) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Lung adenocarcinoma | HCC827 cells | CVCL_2063 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
A total of 250-1500cells (SK-BR-3) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Low ROR1 expression (ROR1+) | ||
| Method Description |
A total of 250-1500cells (MCF-7) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
References