Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ONLOB
ADC Name
WO2021044208A1 ADC 2A2-4
Synonyms
WO2021044208A1 ADC 2A2-4
   Click to Show/Hide
Organization
LegoChem Biosciences, Inc.; ABL Bio, Inc.
Drug Status
Investigative
Indication
In total 3 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Lung cancer [ICD11:2C25]
Investigative
Mantle cell lymphoma [ICD11:2A85]
Investigative
Drug-to-Antibody Ratio
2
Structure
Antibody Name
Anti-ROR1 mAb 2A2
  Antibody Info 
Antigen Name
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
WO2021044208A1_ADC 2A2-4 linker
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 49.63
%
Calu-3 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Calu-3 cells
Lung adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
1000
pM
MDA-MB-231 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.48
nM
JeKo-1 cells
Mantle cell lymphoma
Half Maximal Inhibitory Concentration (IC50) 
> 10
nM
NCI-H2228 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 10
nM
MCF-7 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
23.43
nM
HCC1806 cells
Breast squamous cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 49.63% (Day 26) Positive ROR1 expression (ROR1+++/++)
Method Description
1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 0.25 mg/kg of 2A2 dPBD ADC.
In Vivo Model Calu-3 CDX model
In Vitro Model Lung adenocarcinoma Calu-3 cells CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 26) Positive ROR1 expression (ROR1+++/++)
Method Description
1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 1 mg/kg of 2A2 dPBD ADC.
In Vivo Model Calu-3 CDX model
In Vitro Model Lung adenocarcinoma Calu-3 cells CVCL_0609
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1000 pM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.48 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 23.43 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
References
Ref 1 Antibody-drug conjugate comprising antibody against human ror1, and use for the same; 2021-04-01.

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