Linker Information

General Information of This Linker

Linker ID	LIN0LGSKX
Linker Name	BCN-HydraSpace-Val-Cit-PABC
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
Structure	3D MOL		2D MOL
Formula	C58H88N14O21S2
Isosmiles	CC(C)C(NC(=O)OCCN(CCOC(=O)NC(C(=O)NC(CCCNC(N)=O)C(=O)Nc1ccc(CO)cc1)C(C)C)S(=O)(=O)NC(=O)OCCOCCNS(=O)(=O)NC(=O)OCC1C2CCC#CCCC21)C(=O)NC(CCCNC(N)=O)C(=O)Nc1ccc(CO)cc1
InChI	InChI=1S/C58H88N14O21S2/c1-36(2)47(51(77)66-45(13-9-23-61-53(59)79)49(75)64-40-19-15-38(33-73)16-20-40)68-55(81)90-29-26-72(95(87,88)71-58(84)92-32-31-89-28-25-63-94(85,86)70-57(83)93-35-44-42-11-7-5-6-8-12-43(42)44)27-30-91-56(82)69-48(37(3)4)52(78)67-46(14-10-24-62-54(60)80)50(76)65-41-21-17-39(34-74)18-22-41/h15-22,36-37,42-48,63,73-74H,7-14,23-35H2,1-4H3,(H,64,75)(H,65,76)(H,66,77)(H,67,78)(H,68,81)(H,69,82)(H,70,83)(H,71,84)(H3,59,61,79)(H3,60,62,80)
InChIKey	YDMOZXGNBSQAPE-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	1381.553	Polar area	513.2
	Complexity	95	xlogp Value	-0.0936
	Heavy Count	95	Rot Bonds	40
	Hbond acc	21	Hbond Donor	15

Each Antibody-drug Conjugate Related to This Linker

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

Trastuzumab-SYNtansine [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.60% (Day 23)	High HER2 expression (HER2+++)
Method Description	25 mice with T226 tumor (P12.1.4/0) between 75 and 196 mm³ were allocated, according to their tumor volume to give homogenous mean and median tumor volume in each treatment arm (5 mice/group). Treatments were initiated when the median tumor volume was 126 mm³ by intravenous injection with either vehicle (control), and trastuzumab-SYNtansine 3 mg/kg. Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: T226)
Experiment 2 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 23)	High HER2 expression (HER2+++)
Method Description	25 mice with T226 tumor (P12.1.4/0) between 75 and 196 mm³ were allocated, according to their tumor volume to give homogenous mean and median tumor volume in each treatment arm (5 mice/group). Treatments were initiated when the median tumor volume was 126 mm³ by intravenous injection with either vehicle (control), and trastuzumab-SYNtansine 9 mg/kg. Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: T226)

References

Ref 1	Enzymatic glycan remodeling-metal free click (GlycoConnect) provides homogenous antibody-drug conjugates with improved stability and therapeutic index without sequence engineering. MAbs. 2022 Jan-Dec;14(1):2078466.