Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0DLYRE
ADC Name	FOLR1-ADC 13c
Synonyms	FOLR1 ADC 13c Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Cervical cancer [ICD11:2C77] Investigative Ovarian cancer [ICD11:2C73] Investigative
Drug-to-Antibody Ratio	3.3
	3D MOL	2D MOL
Antibody Name	Anti-FOLR1 mAb		Antibody Info
Antigen Name	Folate receptor alpha (FOLR1)		Antigen Info
Payload Name	PBD dimer 13c		Payload Info
Therapeutic Target	Human Deoxyribonucleic acid (hDNA)		Target Info
Linker Name	Adipic acid-Val-Ala-PABC		Linker Info
Conjugate Type	Random conjugation through nucleophilic lysines.

General Information of The Activity Data Related to This ADC

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)	20	pM	KB cells	Human papillomavirus-related endocervical adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.3	nM	T-47D 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 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 pM	Positive FOLR1 expression (FOLR1+++/++)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	Negative FOLR1 expression (FOLR1-)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

References

Ref 1	Synthesis of Highly Potent N-10 Amino-Linked DNA-Alkylating Indolinobenzodiazepine Antibody-Drug Conjugates (ADCs). ACS Med Chem Lett. 2019 Jul 22;10(8):1211-1215. doi: 10.1021/acsmedchemlett.9b00254. eCollection 2019 Aug 8.