Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0CGCDG
ADC Name	ADC14-0810
Synonyms	Erbitux(LC)-G7CVIM-LBG-MMAF Click to Show/Hide
Organization	LegoChem Biosciences, Inc.
Drug Status	Investigative
Indication	In total 3 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Lung cancer [ICD11:2C25] Investigative Skin squamous cell carcinoma [ICD11:2C31] Investigative
Drug-to-Antibody Ratio	2
Structure
	3D MOL	2D MOL
Antibody Name	Cetuximab (LC) G7-CVIM		Antibody Info
Antigen Name	Epidermal growth factor receptor (EGFR)		Antigen Info
Payload Name	Monomethyl auristatin F		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	ADC14-0810 linker
Conjugate Type	Site-specific conjugation through the CaaX sequence at the C-terminal.

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 (IC50)	0.25	nM	HCC827 cells	Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	6.54	nM	A431 cells	Skin squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	MCF-7 cells	Invasive breast 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 (IC50)	0.25 nM	Moderate EGFR expression (EGFR ++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. The cells were incubated at 37°C in 5% CO₂, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.54 nM	High EGFR expression (CD19 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. The cells were incubated at 37°C in 5% CO₂, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low EGFR expression (EGFR +)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. The cells were incubated at 37°C in 5% CO₂, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

References

Ref 1	Compositions and methods related to anti-egfr antibody drug conjugates; 2017-03-30.