Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0AWDSI
ADC Name	3A5-mc-VC-PAB-MMAE
Synonyms	3A5 mc VC PAB MMAE Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Ovarian cancer [ICD11:2C73] Investigative
Drug-to-Antibody Ratio	2.2
	3D MOL	2D MOL
Antibody Name	Anti-MUC16 Anti-ody 3A5		Antibody Info
Antigen Name	Mucin-16 (MUC16)		Antigen Info
Payload Name	Monomethyl auristatin E		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Mc-Val-Cit-PABC		Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.
Combination Type	Vedotin

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 100	%	OVCAR-3 cells	Ovarian serous adenocarcinoma

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)	0.82	nM	OVCAR-3 cells	Ovarian serous adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	HEK293 cells	Normal

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 50)	Positive MUC16 expression (MUC16 +++/++)
Method Description	In vivo efficacy of MUC16 targeting ADCs in the Ovcar3 tumor model. 3A5-mc-VC-PAB-MMAE ADC dosed at 5 mg/kg (in each study with the exact dosing for control) IV in SCID mice.
In Vivo Model	OVCR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

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)	0.82 nM	Positive MUC16 expression (MUC16 +++/++)
Method Description	Cells were seeded in 96 well plates at 3000 cells per well in complete growth media and grown overnight. For cell viability curves, serially diluted conjugates or payloads were added to the cells at final concentrations ranging from 300 nM to 5 pM and incubated for 8 days.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative MUC16 expression (MUC16-)
Method Description	Cells were seeded in 96 well plates at 3000 cells per well in complete growth media and grown overnight. For cell viability curves, serially diluted conjugates or payloads were added to the cells at final concentrations ranging from 300 nM to 5 pM and incubated for 8 days.
In Vitro Model	Normal	HEK293 cells		CVCL_0045

References

Ref 1	Antibody drug conjugates of cleavable amino-benzoyl-maytansinoids. Bioorg Med Chem. 2020 Dec 1;28(23):115785. doi: 10.1016/j.bmc.2020.115785. Epub 2020 Oct 11.