ADC ID	DRG0SYEBP
ADC Name	WO2025019787A1 ADC-8
Synonyms	WO2025019787A1 ADC-8    Click to Show/Hide
Organization	EXELIXIS, INC.
Drug Status	Investigative
Drug-to-Antibody Ratio	8
Structure
	3D MOL			2D MOL
Antibody Name	A27					Antibody Info
Antigen Name	Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)					Antigen Info
Payload Name	ADC-4 Payload					Payload Info
Linker Name	ADC-4 Linker					Linker Info
Conjugate Type	Conjugation site: CH1/CT
Combination Type	IIa

Standard Type	Value	Units	Description	Reference
Maximum Observed Concentration (Cmax)	114	ug/mL	Sprague-Dawley rats dosed intravenously with a single dose of 5 mg/kg of testd ADC-8 after 16 hours of fasting. 100 uL plasma was collected at 30 min (on Day 0), 6 h (on Day 0), 24 h (on Day1), 48 h (on Day 2), Day 4, Day 7, Day 10, and Day14.    Click to Show/Hide	[1]
Area Under the Concentration-Time Curve (AUC)	368	ug*day/mL	Sprague-Dawley rats dosed intravenously with a single dose of 5 mg/kg of testd ADC-8 after 16 hours of fasting. 100 uL plasma was collected at 30 min (on Day 0), 6 h (on Day 0), 24 h (on Day1), 48 h (on Day 2), Day 4, Day 7, Day 10, and Day14.    Click to Show/Hide	[1]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	368	ug*day/mL	Sprague-Dawley rats dosed intravenously with a single dose of 5 mg/kg of testd ADC-8 after 16 hours of fasting. 100 uL plasma was collected at 30 min (on Day 0), 6 h (on Day 0), 24 h (on Day1), 48 h (on Day 2), Day 4, Day 7, Day 10, and Day14.    Click to Show/Hide	[1]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	368	ug*day/mL	Sprague-Dawley rats dosed intravenously with a single dose of 5 mg/kg of testd ADC-8 after 16 hours of fasting. 100 uL plasma was collected at 30 min (on Day 0), 6 h (on Day 0), 24 h (on Day1), 48 h (on Day 2), Day 4, Day 7, Day 10, and Day14.    Click to Show/Hide	[1]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	368	ug*day/mL	Sprague-Dawley rats dosed intravenously with a single dose of 5 mg/kg of testd ADC-8 after 16 hours of fasting. 100 uL plasma was collected at 30 min (on Day 0), 6 h (on Day 0), 24 h (on Day1), 48 h (on Day 2), Day 4, Day 7, Day 10, and Day14.    Click to Show/Hide	[1]
Clearance (CL)	13.8	mL/day/kg	Sprague-Dawley rats dosed intravenously with a single dose of 5 mg/kg of testd ADC-8 after 16 hours of fasting. 100 uL plasma was collected at 30 min (on Day 0), 6 h (on Day 0), 24 h (on Day1), 48 h (on Day 2), Day 4, Day 7, Day 10, and Day14.    Click to Show/Hide	[1]
Elimination Half-Life (t1/2)	3.3	day	Sprague-Dawley rats dosed intravenously with a single dose of 5 mg/kg of testd ADC-8 after 16 hours of fasting. 100 uL plasma was collected at 30 min (on Day 0), 6 h (on Day 0), 24 h (on Day1), 48 h (on Day 2), Day 4, Day 7, Day 10, and Day14.    Click to Show/Hide	[1]

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal inhibitory Concentration (lC50)	0.318	nM	CVCL_0045	Normal

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.318 nM	Positive huROR1 expression (huROR1+++/++)
Method Description	ADC-8 was tested in HEK293-huROR1 cells, starting with a top concentration of 60 nM (4x the final top concentration),each of the samples was serially diluted 5 times (1:4 for ADC-8), 5 days.
In Vitro Model	Normal	HEK293-huROR1 cells		CVCL_0045

Ref 1	Tyrosine-protein kinase membrane receptor 1 (ROR1) antibody-drug conjugates and uses thereof