Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0UXHIX
ADC Name
EP4471061A1 MC_Dxd
Synonyms
EP4471061A1 MC_Dxd
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Organization
Emergence Therapeutics AG
Drug Status
Investigative
Antibody Name
huASCT2 17c10 mAb
  Antibody Info 
Antigen Name
Amino acid transporter (ASCT2)
  Antigen Info 
Payload Name
DX-8951 derivative (DXd)
  Payload Info 
Therapeutic Target
DNA topoisomerase 1 (TOP1)
  Target Info 
Linker Name
6-Maleimidocaproic acid
  Linker Info 
Combination Type
MC-Dxd
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
9- 4.6 × 10 -4
ug/mL
CVCL_0291
Colon carcinoma
Half Maximal inhibitory Concentration (lC50) 
9- 4.6 × 10 -4
ug/mL
CVCL_2760
Colon adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 9- 4.6 × 10 -4 ug/mL Positive ASCT2 expression (ASCT2+++/++)
Method Description
Target cells were seeded in triplicates into flat-bottom 384-wells plate (400 cells for HCT116 cells). Cells were incubated for 3 to 4 hours at 37°C before addition of an equivalent volume of 2X concentrated ADC or free drug-linker dose range (see table 1 for details). Cells were then incubated into a live cell imaging instrument (Incucyte®) for 6 to 8 days and their confluency was monitored all along the culture.

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In Vitro Model Colon carcinoma HCT116 cells CVCL_0291
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 9- 4.6 × 10 -4 ug/mL Positive ASCT2 expression (ASCT2+++/++)
Method Description
Target cells were seeded in triplicates into flat-bottom 384-wells plate (400 cells for HCT116 cells). Cells were incubated for 3 to 4 hours at 37°C before addition of an equivalent volume of 2X concentrated ADC or free drug-linker dose range (see table 1 for details). Cells were then incubated into a live cell imaging instrument (Incucyte®) for 6 to 8 days and their confluency was monitored all along the culture.

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In Vitro Model Colon adenocarcinoma WiDr cells CVCL_2760
References
Ref 1 Anti-ASCT2 antibodies and ADCs derived therefrom