Payload Information

General Information of This Payload

Payload ID	PAY0UYNEC
Name	WL-14
Synonyms	WL-14 Click to Show/Hide
Target	DNA topoisomerase I (TOP1)			Target Info
Formula	C28H23N3O7
Isosmiles	O=C1OCC(C2=O)=C(C=C3C4=NC5=CC6=C(OCO6)C=C5C(C7=CC=NC=C7)=C4CN23)[C@](O)([C@@H]1OC)CC
InChI	InChI=1S/C28H23N3O7/c1-3-28(34)18-9-20-24-16(11-31(20)26(32)17(18)12-36-27(33)25(28)35-2)23(14-4-6-29-7-5-14)15-8-21-22(38-13-37-21)10-19(15)30-24/h4-10,25,34H,3,11-13H2,1-2H3/t25-,28+/m1/s1
InChIKey	DPNMWCZJIUYTOP-NAKRPHOHSA-N
Pharmaceutical Properties	Molecule Weight	513.506	Polar area	122
	Complexity	1675.689369	xlogp Value	2.8853
	Heavy Count	38	Rot Bonds	3
	Hbond acc	10	Hbond Donor	1

The activity data of This Payload

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	<0.013	nM	MDA-MB-468 cells	Breast adenocarcinoma	CVCL_0419	[1]
Half Maximal Inhibitory Concentration (IC50)	<0.013	nM	MDA-MB-468 cells	Breast adenocarcinoma	CVCL_0419	[1]
Half Maximal Inhibitory Concentration (IC50)	<0.013	nM	NCI-N87 cells	Gastric tubular adenocarcinoma	CVCL_1603	[1]
Half Maximal Inhibitory Concentration (IC50)	<0.013	nM	NCI-N87 cells	Gastric tubular adenocarcinoma	CVCL_1603	[1]
Half Maximal Inhibitory Concentration (IC50)	<0.013	nM	SK-BR-3 cells	Breast adenocarcinoma	CVCL_0033	[1]
Half Maximal Inhibitory Concentration (IC50)	<0.013	nM	SK-BR-3 cells	Breast adenocarcinoma	CVCL_0033	[1]

Each Antibody-drug Conjugate Related to This Payload

Full Information of The Activity Data of The ADC(s) Related to This Payload

HER2-11 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	77.81 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	Cells were plated into 96-well white round-bottom plates in RPMI-1640 medium supplemented with 10 % FBS. 24 h later, compounds were added to the 96-well plates. Following a 120h incubation period, cell viability was evaluated by a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) and the EC50 values of each compound were determined. Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

HER2-18 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	67.94&#17713.53 ng/mL	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	Cells were distributed into 96-well white round-bottom plates, with each well receiving 1000 cells in RPMI-1640 medium supplemented with 10% FBS. Following a 24-hour incubation period, diluted compounds were introduced to the wells. After 144 hours, a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) was performed to assess cell viability. The luminescent readings were normalized as percentages relative to untreated cells, and the IC50 values for each compound were determined. Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

HER2-17 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	142.21&#17726.91 ng/mL	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	Cells were distributed into 96-well white round-bottom plates, with each well receiving 1000 cells in RPMI-1640 medium supplemented with 10% FBS. Following a 24-hour incubation period, diluted compounds were introduced to the wells. After 144 hours, a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) was performed to assess cell viability. The luminescent readings were normalized as percentages relative to untreated cells, and the IC50 values for each compound were determined. Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

References

Ref 1	Synthesis and biological evaluation of novel quaternary ammonium antibody drug conjugates based on camptothecin derivatives
Ref 2	Comparison of quaternary ammonium-based linkers for antibody-drug conjugates based on camptothecin derivatives