General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0SYIAO
ADC Name
WO2024092067A1 ADC 2E7-LD038 (PA038)
Synonyms
PA038
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Organization
PROFOUNDBIO US CO.
Drug Status
Investigative
Antibody Name
20000000
 Antibody Info 
Antigen Name
CD70 antigen (CD70)
 Antigen Info 
Payload Name
Undisclosed
Therapeutic Target
Stimulator of interferon genes protein (STING1)
 Target Info 
Linker Name
Drug linker PB038
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Special Approval(s)
Investigative
ADC-specific functional property(2027 Update)
Circulating Stability
Click To Hide/Show 1 ADC-specific functional property Data
Incubation Time 15days Release Undisclosed Reference
[1]
Description
When stored at 37°C for up to 15 days or undergoing 5 cycles of freeze-thaw, ADC PA038 appeared to be stable by both HIC and SEC. No significant increase in aggregation was observed overtime at 37°C or multiple freeze-thaw cycles.

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General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
36
nM
CVCL_0511
EBV-related Burkitt lymphoma
Half Maximal inhibitory Concentration (lC50) 
37
nM
CVCL_0234
Clear cell renal cell carcinoma
Half Maximal inhibitory Concentration (lC50) 
292
nM
CVCL_1051
Renal cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 36 nM Moderate CD70 expression (CD70++)
Method Description
Cell Raji were cultured in CO2, thermostatic incubator at 37°C with 5% CO2, in standard conditions. Cells were sub-cultured every 1-2 days, digested with 0.25% trypsin and passaged with a suitable density. When the cells were in the logarithmic growth phase and the amount meeting the assay's demand, cells were collectedand plated onto 96-well solid white flat bottom plates for assay. One day later test articles 2E7-LD038 conjugate ranging from 2 uM to 0.1nM, or extecan ranging from 20 uM to 0.03 nM were added to the cells. Plates were then incubated at 37°C for 96h. Cell Titer Glo (CTG) (40 ul per well) was subsequently added to the plates. Luciferase reading was collected 5min after and analyzed by Microplatereaders. All readings were normalized as percentage of viable cells in the untreated control wells and theICso yalues were calculated by Prism software.

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In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
37 nM
Method Description
Cell Caki-1 were cultured in CO2, thermostatic incubator at 37°C with 5% CO2, in standard conditions. Cells were sub-cultured every 1-2 days, digested with 0.25% trypsin and passaged with a suitable density. When the cells were in the logarithmic growth phase and the amount meeting the assay's demand, cells were collectedand plated onto 96-well solid white flat bottom plates for assay. One day later test articles 2E7-LD038 conjugate ranging from 2 uM to 0.1nM, or extecan ranging from 20 uM to 0.03 nM were added to the cells. Plates were then incubated at 37°C for 96h. Cell Titer Glo (CTG) (40 ul per well) was subsequently added to the plates. Luciferase reading was collected 5min after and analyzed by Microplatereaders. All readings were normalized as percentage of viable cells in the untreated control wells and theICso yalues were calculated by Prism software.

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In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
292 nM
Method Description
Cell 786-O were cultured in CO2, thermostatic incubator at 37°C with 5% CO2, in standard conditions. Cells were sub-cultured every 1-2 days, digested with 0.25% trypsin and passaged with a suitable density. When the cells were in the logarithmic growth phase and the amount meeting the assay's demand, cells were collectedand plated onto 96-well solid white flat bottom plates for assay. One day later test articles 2E7-LD038 conjugate ranging from 2 uM to 0.1nM, or extecan ranging from 20 uM to 0.03 nM were added to the cells. Plates were then incubated at 37°C for 96h. Cell Titer Glo (CTG) (40 ul per well) was subsequently added to the plates. Luciferase reading was collected 5min after and analyzed by Microplatereaders. All readings were normalized as percentage of viable cells in the untreated control wells and theICso yalues were calculated by Prism software.

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In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
References
Ref 1 CD70 antibody drug conjugates and methods of using the same