Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0LKHDN
ADC Name	Homo-Ang2-Cys5.5 conjugate DAR 4
Synonyms	Homo Ang2 Cys5.5 conjugate DAR 4; Homogeneous Ang2 conjugate DAR 4 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Glioblastoma [ICD11:2A00] Investigative
Drug-to-Antibody Ratio	4
	3D MOL	2D MOL
Antibody Name	Anti-EGFRvIII mAb		Antibody Info
Antigen Name	Epidermal growth factor receptor variant III (EGFRvIII)		Antigen Info
Payload Name	Angiopep-2 TFA		Payload Info
Linker Name	Mal-DBCO-PEG3		Linker Info
Conjugate Type	Site-specific conjugation through the glutamine 296 by an engineered transglutaminase (mTgase).

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)	77.2	nM	U87EGFR-Luc cells	Glioblastoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	U87EGFR-Luc cells	Glioblastoma
Half Maximal Inhibitory Concentration (IC50)	80.8	%	U87EGFR-Luc cells	Glioblastoma

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)	77.20 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	ADC cell viability assay in U87EGFR-Luc (EGFRvIII+ ) and HEK293 (EGFRvIII - ) cells.
In Vitro Model	Glioblastoma	U87EGFR-Luc cells		CVCL_0022
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR vIII expression (EGFR vIII-)
Method Description	ADC cell viability assay in U87EGFR-Luc (EGFRvIII+ ) and HEK293 (EGFRvIII - ) cells.
In Vitro Model	Glioblastoma	U87EGFR-Luc cells		CVCL_0022
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.80%	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	ADC cell viability assay in U87EGFR-Luc (EGFRvIII+ ) and HEK293 (EGFRvIII - ) cells.
In Vitro Model	Glioblastoma	U87EGFR-Luc cells		CVCL_0022

References

Ref 1	Homogeneous antibody-angiopep 2 conjugates for effective brain targeting. RSC Adv. 2022 Jan 26;12(6):3359-3364.