Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0LXEXH
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| ADC Name |
C4.4A-EC5
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| Synonyms |
C4.4a EC5; C4.4aEC5
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| Drug Status |
Investigative
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| Indication |
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Lung cancer [ICD11:2C25]
Investigative
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| Drug-to-Antibody Ratio |
3.6
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| Structure |
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| Antibody Name |
Anti-human LYPD3 mAb
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Antibody Info | ||||
| Antigen Name |
Ly6/PLAUR domain-containing protein 3 (LYPD3)
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Antigen Info | ||||
| Payload Name |
NAMPT inhibitor 6
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Payload Info | ||||
| Therapeutic Target |
Nicotinamide phosphoribosyltransferase (NAMPT)
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Target Info | ||||
| Linker Name |
Open-chain glycine maleimide-PEG
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Linker Info | ||||
| Conjugate Type |
Glycine maleimide was used for Michael addition reactions with the thiol groups of the antibody that were generated through the reduction of interchain disulfide bonds. Basic opening of the resulting succinimide at pH 8 to obtain an open-chain succinic amide.
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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 (IC50) | 8.40 nM | High LYPD3 expression (LYPD3+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
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| In Vitro Model | Lung adenocarcinoma | A549-C4.4a cells | CVCL_0023 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 48.00 nM | High CD276 expression (CD276+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 uM | High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
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| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
References
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