Linker Information

General Information of This Linker

Linker ID	LIN0YZZJX
Linker Name	Linker of ADC2-51
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
Structure	3D MOL		2D MOL
Formula	C37H51N7O15S
Isosmiles	O=C(NCC(NCC(N[C@@H](CC1=CC=CC=C1)C(NCC(O)=O)=O)=O)=O)[C@@H](NC(CCCCCN2C(C=CC2=O)=O)=O)CCC(NC[C@H](O3)[C@H](O)[C@@H](O)[C@H](O)[C@H]3CO)=O.[S]
InChI	InChI=1S/C37H51N7O15.S/c45-20-25-34(55)35(56)33(54)24(59-25)16-38-26(46)11-10-22(42-27(47)9-5-2-6-14-44-30(50)12-13-31(44)51)36(57)40-17-28(48)39-18-29(49)43-23(37(58)41-19-32(52)53)15-21-7-3-1-4-8-21;/h1,3-4,7-8,12-13,22-25,33-35,45,54-56H,2,5-6,9-11,14-20H2,(H,38,46)(H,39,48)(H,40,57)(H,41,58)(H,42,47)(H,43,49)(H,52,53);/t22-,23-,24-,25+,33-,34+,35+;/m0./s1
InChIKey	AOFMOULFSIJPQV-OOPCOKNSSA-N
Pharmaceutical Properties	Molecule Weight	865.916	Polar area	339.43
	Complexity	1598.298893	xlogp Value	-4.4957
	Heavy Count	60	Rot Bonds	24
	Hbond acc	14	Hbond Donor	11

Each Antibody-drug Conjugate Related to This Linker

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

WO2024110905A1 ADC-C3 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.008 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.018 nM	High B7H3 expression (B7H3 +++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.291 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Negative B7H3 expression (B7H3-)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

WO2024110905A1 ADC-C4 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.018 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.022 nM	High B7H3 expression (B7H3 +++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.291 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Negative B7H3 expression (B7H3-)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

WO2024110905A1 ADC-C5 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.038 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.074 nM	High B7H3 expression (B7H3 +++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.245 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Negative B7H3 expression (B7H3-)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

BGA8357 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.14 nM	Positive CEA expression (CEA+++/++)
Method Description	NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.38 nM	Positive CEA expression (CEA+++/++)
Method Description	MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.67 nM	Positive CEA expression (CEA+++/++)
Method Description	Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Colon adenocarcinoma	Ls147T cells		CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	26 nM	Negative CEA expression (CEA-)
Method Description	MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

References

Ref 1	Antibody drug conjugates
Ref 2	Anti-CEA antibody drug conjugates and methods of use