Linker Information

General Information of This Linker

Linker ID	LIN0PCMIJ
Linker Name	Gal-beta-1,4-GlcNAc
Linker Type	Glycosidases-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
Structure	3D MOL		2D MOL
Formula	C52H87N7O23
Isosmiles	CC1=NC2C(O1)OC(CO)C(OC1OC(COCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NC(C(=O)NC(CCCNC(N)=O)C(=O)Nc3ccc(CO)cc3)C(C)C)C(O)C(O)C1O)C2O
InChI	InChI=1S/C52H87N7O23/c1-32(2)41(49(69)58-36(5-4-12-55-52(53)70)48(68)57-35-8-6-34(29-60)7-9-35)59-40(63)11-15-72-18-21-75-24-26-76-25-23-74-20-17-71-14-10-39(62)54-13-16-73-19-22-77-27-28-78-31-38-43(64)45(66)46(67)51(81-38)82-47-37(30-61)80-50-42(44(47)65)56-33(3)79-50/h6-9,32,36-38,41-47,50-51,60-61,64-67H,4-5,10-31H2,1-3H3,(H,54,62)(H,57,68)(H,58,69)(H,59,63)(H3,53,55,70)
InChIKey	UBMDLCFDEOENNJ-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	1178.294	Polar area	416.02
	Complexity	82	xlogp Value	-3.6912
	Heavy Count	82	Rot Bonds	43
	Hbond acc	24	Hbond Donor	12

Each Antibody-drug Conjugate Related to This Linker

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

Trastuzumab-Gal-beta-1,4GlcNAc-MMAE [Investigative]

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 Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 nM 6.08 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 nM 11.07 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

References

Ref 1	Synthesis and Evaluation of Three Azide-Modified Disaccharide Oxazolines as Enzyme Substrates for Single-Step Fc Glycan-Mediated Antibody-Drug Conjugation. Bioconjug Chem. 2022 Jun 15;33(6):1179-1191.