Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0FJFAH
ADC Name	H3L2-mpeoDM1
Synonyms	JmD4 Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Lung cancer [ICD11:2C25] Investigative
Drug-to-Antibody Ratio	3.96
	3D MOL	2D MOL
Antibody Name	Anti-DLL4 mAb H3L2		Antibody Info
Antigen Name	Delta-like protein 4 (DLL4)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	BIMPRO		Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 2 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 84.38	%	A-549 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 88.43	%	MDA-MB-231 cells	Breast adenocarcinoma

Revealed Based on the Cell Line Data

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

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	36.12	nM	HUVEC-C cells	Normal

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.38% (Day 24)	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg JmD4 was intravenously administered once every three days for three weeks.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.43% (Day 24)	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg JmD4 was intravenously administered once every three days for three weeks.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	36.12 nM	Positive DLL4 expression (DLL4 +++/++)
Method Description	In vitro cytotoxicity and mechanism of anti-DLL4 ADCs. The cytotoxicity of ADCs was assessed by MTT assay. The percentage of cell inhibition relative to untreated control HUVEC cells was calculated for each drug concentration.
In Vitro Model	Normal	HUVEC-C cells		CVCL_2959

References

Ref 1	Two engineered site-specific antibody-drug conjugates, HLmD4 and HLvM4, have potent therapeutic activity in two DLL4-positive tumour xenograft models. Am J Cancer Res. 2020 Aug 1;10(8):2387-2408. eCollection 2020.