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Each Antibody-drug Conjugate Related to This Payload

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WO2022078260A1 ADC-1 [Investigative]

ADC Info

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)	≈ 68.00% (Day 31)	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish gastric tubular adenocarcinoma model, 5 x 10⁶ cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm³ mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

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)	14.79 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.59 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

References

Ref 1	Camptothecin derivative and ligand-drug conjugate thereof; 2022-04-21.