Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0LDXSO
ADC Name	TWEAKR-KSP-ADC 2.1
Synonyms	TWEAKR-KSP-ADC-2.1 Click to Show/Hide
Drug Status	Investigative
Indication	In total 3 Indication(s) Colorectal cancer [ICD11:2B91] Investigative Non-small cell lung cancer [ICD11:2C25] Investigative Pancreatic cancer [ICD11:2C10] Investigative
Drug-to-Antibody Ratio	2.1
	3D MOL	2D MOL
Antibody Name	Anti-TWEAKR mAb		Antibody Info
Antigen Name	Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)		Antigen Info
Payload Name	Pyrrole based kinesin spindle protein inhibitor		Payload Info
Therapeutic Target	Kinesin-like protein KIF11 (KIF11)		Target Info
Linker Name	Kinesin spindle protein inhibitor (KSPi)-ADC linker 5		Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.

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)	0.06	nM	LoVo cells	Colon adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.16	nM	BxPC-3 cells	Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.31	nM	NCI-H292 cells	Lung mucoepidermoid carcinoma

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)	0.06 nM	High TWEAKR expression (TWEAKR +++)
Method Description	In vitro potency of SMOL KSPi compound A and of TWEAKR-KSPiADCs 1.1., 1.2, 1.3, 1.4, 2.1, and 2.2 in TWEAKR-expressing cell lines versus selected respective isotype control ADCs 1.4 and 2.2 with same linker payload chemistry.
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	High TWEAKR expression (TWEAKR +++)
Method Description	In vitro potency of SMOL KSPi compound A and of TWEAKR-KSPiADCs 1.1., 1.2, 1.3, 1.4, 2.1, and 2.2 in TWEAKR-expressing cell lines versus selected respective isotype control ADCs 1.4 and 2.2 with same linker payload chemistry.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	High TWEAKR expression (TWEAKR +++)
Method Description	In vitro potency of SMOL KSPi compound A and of TWEAKR-KSPiADCs 1.1., 1.2, 1.3, 1.4, 2.1, and 2.2 in TWEAKR-expressing cell lines versus selected respective isotype control ADCs 1.4 and 2.2 with same linker payload chemistry.
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455

References

Ref 1	Antibody-Drug Conjugates with Pyrrole-Based KSP Inhibitors as the Payload Class. Angew Chem Int Ed Engl. 2018 Nov 12;57(46):15243-15247. doi: 10.1002/anie.201807619. Epub 2018 Oct 15.