Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0WPOCV
ADC Name
38139459 8D302-DXd
Synonyms
8D302-DXd
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Organization
Engineering Research Center of Cell & Therapeutic Antibody, Ministry of Education, School of Pharmacy, Shanghai Jiao Tong University,.
Drug Status
Investigative
Drug-to-Antibody Ratio
7.57
Structure
Antibody Name
8D302
  Antibody Info 
Antigen Name
Sortilin (SORT1)
  Antigen Info 
Payload Name
DX-8951 derivative (DXd)
  Payload Info 
Therapeutic Target
DNA topoisomerase 1 (TOP1)
  Target Info 
Linker Name
Mc-Gly-Gly-Phe-Gly
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The ADMET Data Related to This ADC(2027 Update)
Excretion
Click To Hide/Show 1 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Elimination Half-Life (t1/2) 168 h
The pharmacokinetics profile was evaluated in BALB/c mice with a 5 mg/kg dose of 8D302-MMAE or 8D302-DXd.
 [1]
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) 
2.05
nM
CVCL_0553
Invasive breast carcinoma of no special type
Half Maximal inhibitory Concentration (lC50) 
24.07
nM
CVCL_0031
Invasive breast carcinoma
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) 2.05 nM Moderate SORT1 expression (SORT1++)
Method Description
The in vitro cell-killing assay was carried out using MDA-MB-231, MCF-7, MCF-10A, and T47D. Cells were plated in 96-well plates (5000 cells/well). After 1 h incubation, ADCs were added in a serial of concentrations with three replicates per concentration. The concentration of ADCs against MDA-MB-231, MCF-7, and MCF-10A ranged from 300 nM to 137 pM, while the range of concentration was from 100 nM to 46 pM for T47D. This was followed by another 72 h of culture. Cell viability was detected using the Cell Counting Kit 8 (APExBIO, Houston, TX, USA).

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In Vitro Model Invasive breast carcinoma of no special type T47D cells CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 24.07 nM Moderate SORT1 expression (SORT1++)
Method Description
The in vitro cell-killing assay was carried out using MDA-MB-231, MCF-7, MCF-10A, and T47D. Cells were plated in 96-well plates (5000 cells/well). After 1 h incubation, ADCs were added in a serial of concentrations with three replicates per concentration. The concentration of ADCs against MDA-MB-231, MCF-7, and MCF-10A ranged from 300 nM to 137 pM, while the range of concentration was from 100 nM to 46 pM for T47D. This was followed by another 72 h of culture. Cell viability was detected using the Cell Counting Kit 8 (APExBIO, Houston, TX, USA).

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Generation and Characterization of SORT1-Targeted Antibody-Drug Conjugate for the Treatment of SORT1-Positive Breast Tumor