Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0PZEQO
ADC Name	T-DM1-2.6
Synonyms	T-DM1 DAR2.6 Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Gastric cancer [ICD11:2B72] Investigative
Drug-to-Antibody Ratio	2.6
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)		Linker Info
Conjugate Type	Random conjugation through nucleophilic lysines.
Combination Type	Emtansine

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)	0.04	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	1.05	nM	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 66	nM	MDA-MB-231 cells	Breast adenocarcinoma

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)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO₂ cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO₂ cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO₂ cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

References

Ref 1	Hiding Payload Inside the IgG Fc Cavity Significantly Enhances the Therapeutic Index of Antibody-Drug Conjugates. J Med Chem. 2023 Jan 12;66(1):1011-1026. doi: 10.1021/acs.jmedchem.2c01812. Epub 2022 Dec 30.