Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0VPKXB
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| ADC Name |
aPDL1-NPLG-SN38
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| Synonyms |
aPDL1-NPLG-SN38
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| Organization |
Key Laboratory of Environmentally Friendly Chemistry and Applications of Ministry of Education and Key Laboratory of Polymeric Materials & Application Technology of Hunan Province, Xiangtan University, Xiangtan, 411105, PR China; Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, China.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
72
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| Structure |
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| Antibody Name |
undisclosed
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| Antigen Name |
Programmed cell death 1 ligand 1 (CD274)
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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 |
NPLG
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Linker Info | ||||
| Conjugate Type |
Site-specific bioconjugation via Ultrahigh-DAR platform.
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ADC-specific functional property(2027 Update)
Payload Release Efficiency
| Incubation Time | 72h | Release | 22% | Reference |
[1]
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| Description |
The SN38 release of aPDL1-NPLG-SN38 in deionized water (DIW), 10% serum, or PBS buffer (pH 7.4, with or without esterase) at 37 °C was measured after dialysis. As shown in Fig. 1E, 22.0% and 51.0% of SN38 from aPDL1-NPLG-SN38 released in deionized water and serum within 72 h, respectively, while 64.8% of SN38 released in PBS without esterase. However, the SN38 release rate of was 93.1% in the presence of esterase (20 U mL-1). The results demonstrated that the ester bonds in aPDL1-NPLG-SN38 were cleaved by esterase, allowing the release of SN38 at the site of a tumor.
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| Incubation Time | 72h | Release | 51% | Reference |
[1]
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| Description |
The SN38 release of aPDL1-NPLG-SN38 in deionized water (DIW), 10% serum, or PBS buffer (pH 7.4, with or without esterase) at 37 °C was measured after dialysis. As shown in Fig. 1E, 22.0% and 51.0% of SN38 from aPDL1-NPLG-SN38 released in deionized water and serum within 72 h, respectively, while 64.8% of SN38 released in PBS without esterase. However, the SN38 release rate of was 93.1% in the presence of esterase (20 U mL-1). The results demonstrated that the ester bonds in aPDL1-NPLG-SN38 were cleaved by esterase, allowing the release of SN38 at the site of a tumor.
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| Incubation Time | 72h | Release | 64.8% | Reference |
[1]
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| Description |
The SN38 release of aPDL1-NPLG-SN38 in deionized water (DIW), 10% serum, or PBS buffer (pH 7.4, with or without esterase) at 37 °C was measured after dialysis. As shown in Fig. 1E, 22.0% and 51.0% of SN38 from aPDL1-NPLG-SN38 released in deionized water and serum within 72 h, respectively, while 64.8% of SN38 released in PBS without esterase. However, the SN38 release rate of was 93.1% in the presence of esterase (20 U mL-1). The results demonstrated that the ester bonds in aPDL1-NPLG-SN38 were cleaved by esterase, allowing the release of SN38 at the site of a tumor.
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| Incubation Time | 72h | Release | 93.1% | Reference |
[1]
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| Description |
The SN38 release of aPDL1-NPLG-SN38 in deionized water (DIW), 10% serum, or PBS buffer (pH 7.4, with or without esterase) at 37 °C was measured after dialysis. As shown in Fig. 1E, 22.0% and 51.0% of SN38 from aPDL1-NPLG-SN38 released in deionized water and serum within 72 h, respectively, while 64.8% of SN38 released in PBS without esterase. However, the SN38 release rate of was 93.1% in the presence of esterase (20 U mL-1). The results demonstrated that the ester bonds in aPDL1-NPLG-SN38 were cleaved by esterase, allowing the release of SN38 at the site of a tumor.
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General Information of The Activity Data Related to This ADC
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 | [2] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 2.27 uM | High PD-L1 expression (PD-L1 +++) | ||
| Method Description |
The cytotoxicity of SN38, IgG-NPLG-SN38 and aPDL1-NPLG-SN38 toward MC38 cells was evaluated using a CCK-8 assay. Specifically, the MC38 cells were seeded into 96-well plates (5 × 103 cells per well) and incubated overnight. SN38, IgG-NPLG-SN38 or aPDL1-NPLG-SN38 was then added at a range of concentrations (0.01-100 uM SN38) to each well and cultured for 72 h. CCK-8 reagent was then added to each well and incubated for 1 h, after which the plate was measured on a microplate reader at a wavelength of 450 nm. Cell viability was calculated from the ratio of optical density (OD) values of sample to control wells.
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| In Vitro Model | Mouse colon adenocarcinoma | MC38 cells | CVCL_B288 | ||
References