Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0OXZTH
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| ADC Name |
EGC-PABC-DuoDM ADC
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| Synonyms |
EGC-PABC-DuoDM ADC
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| Organization |
University of Texas Health Science Center at Houston.; The University of Texas MD Anderson Cancer Center UTHealth Houston Graduate School of Biomedical Sciences.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
H231
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Antibody Info | ||||
| Antigen Name |
Epiregulin (EREG)
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Antigen Info | ||||
| Payload Name |
Duocarmycin DM
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Payload Info | ||||
| Linker Name |
BCN-PEG3-EGC-PABC
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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ADC-specific functional property(2027 Update)
Binding Affinity
| Dissocation Constant (Kd) | Binding Target | Description | Reference |
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| ≈2 nM |
DLD1 cells
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Prior to evaluating therapeutic efficacy, we measured binding of all three EREG ADCs in parallel in DLD1 cells. All ADCs demonstrated comparable binding affinities (Kd≈2.0 nmol/L).
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[1]
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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) | 0.06۪.048 nM | High EREG expression (EREG +++) | ||
| Method Description |
Colorectal cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
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| In Vitro Model | Colon adenocarcinoma | LoVo cells | CVCL_0399 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.19۪.07 nM | High EREG expression (EREG +++) | ||
| Method Description |
Colorectal cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
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| In Vitro Model | Colon carcinoma | HCT116 cells | CVCL_0291 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.38۪.19 nM | High EREG expression (EREG +++) | ||
| Method Description |
Colorectal cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
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| In Vitro Model | Colon adenocarcinoma | DLD-1 cells | CVCL_0248 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.5۪.14 nM | Moderate EREG expression (EREG++) | ||
| Method Description |
Colorectal cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
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| In Vitro Model | Colon adenocarcinoma | SW48 cells | CVCL_1724 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 4.93۬.79 nM | Low EREG expression (EREG+) | ||
| Method Description |
Colorectal cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
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| In Vitro Model | Colon adenocarcinoma | SW620 cells | CVCL_0547 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 31.66䔼.12 nM | Low EREG expression (EREG+) | ||
| Method Description |
Colorectal cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
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| In Vitro Model | Colon carcinoma | RKO cells | CVCL_0504 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 10000 nM | Negative EREG expression (EREG-) | ||
| Method Description |
Colorectal cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
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| In Vitro Model | Colon adenocarcinoma | DLD-1 cells (EREG KO) | CVCL_0248 | ||
References