Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0MEYZH
ADC Name	TWEAKR-KSP-ADC 1.1
Synonyms	TWEAKR-KSP-ADC-1.1 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	3
	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 1		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)	0.41	nM	NCI-H292 cells	Lung mucoepidermoid carcinoma
Half Maximal Inhibitory Concentration (IC50)	0.97	nM	BxPC-3 cells	Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	600	nM	LoVo cells	Colon 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)	0.41 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
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 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)	600 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

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.