General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0IKJTH
ADC Name
LCB14-0648
Synonyms
LCB14 0648; ADC14-0610
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Organization
LegoChem Biosciences, Inc.
Drug Status
Investigative
Indication
In total 1 Indication(s)
Burkitt lymphoma [ICD11:2A85]
Investigative
Drug-to-Antibody Ratio
2
Structure
Antibody Name
Anti-CD19 mAb DI-B4
 Antibody Info 
Antigen Name
B-lymphocyte antigen CD19 (CD19)
 Antigen Info 
Payload Name
Monomethyl auristatin F
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
LCB14-0648 linker
Conjugate Type
Site-specific conjugation through the CaaX sequence at the C-terminal.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 80.97
%
Ramos cells
Burkitt lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 85.16
%
Ramos cells
Burkitt lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 88.7
%
Ramos cells
Burkitt lymphoma
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 (IC50) 
110
ng/mL
Raji cells
EBV-related Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50) 
> 10
ug/mL
K562 cells
Chronic myeloid leukemia
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.97% (Day 21) Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 2 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.16% (Day 21) Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 5 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88.70% (Day 21) Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 10 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
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 (IC50) 110 ng/mL Positive CD19 expression (CD19 +++/++)
Method Description
Raji cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
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 (IC50) > 10.00 ug/mL Negative CD19 expression (CD19 -)
Method Description
K562 cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°Cin 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
References
Ref 1 Compositions and methods related to anti-cd19 antibody drug conjugates; 2017-03-30.

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