Linker Information

General Information of This Linker

Linker ID	LIN0EXGPX
Linker Name	Gly5
Linker Type	Sortase-based site-specific conjugation linker
Antibody-Linker Relation	Uncleavable
Structure
Structure	3D MOL		2D MOL
Formula	C10H17N5O6
Isosmiles	C(C(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)O)N
PubChem CID	81537
InChI	InChI=1S/C10H17N5O6/c11-1-6(16)12-2-7(17)13-3-8(18)14-4-9(19)15-5-10(20)21/h1-5,11H2,(H,12,16)(H,13,17)(H,14,18)(H,15,19)(H,20,21)
InChIKey	MXHCPCSDRGLRER-UHFFFAOYSA-N
IUPAC Name	2-[[2-[[2-[[2-[(2-aminoacetyl)amino]acetyl]amino]acetyl]amino]acetyl]amino]acetic acid
Pharmaceutical Properties	Molecule Weight	303.27	Polar area	180
	Complexity	424	xlogp Value	-4.9
	Heavy Count	21	Rot Bonds	9
	Hbond acc	7	Hbond Donor	6

Each Antibody-drug Conjugate Related to This Linker

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

CAC10-Gly5-MAY [Investigative]

ADC Info

Discovered Using Cell Line-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)	≈ 100.00% (Day 14)	High CD30 expression (CD30+++)
Method Description	CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 1 mg/kg preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm³.
In Vivo Model	Non-Hodgkin's lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 16)	High CD30 expression (CD30+++)
Method Description	CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 10 mg/kg ADC preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm³.
In Vivo Model	Non-Hodgkin's lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

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 Inhibitory Concentration (IC50)	4.70 ng/mL	High CD30 expression (CD30+++)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO₂ atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

CAC10-Gly5-PNU [Investigative]

ADC Info

Discovered Using Cell Line-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)	≈ 100.00% (Day 16)	High CD30 expression (CD30+++)
Method Description	CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 1 mg/kg preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm³.
In Vivo Model	Non-Hodgkin's lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 14)	High CD30 expression (CD30+++)
Method Description	CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 1 mg/kg preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm³.
In Vivo Model	Non-Hodgkin's lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.80 ng/mL	High CD30 expression (CD30+++)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO₂ atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.80 ng/mL	Negative CD30 expression (CD30-)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO₂ atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	B acute lymphoblastic leukemia	Reh cells		CVCL_1650

Tras-Gly5-May [Investigative]

ADC Info

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO₂ atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 110.00 ng/mL	Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO₂ atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

References

Ref 1	Highly Potent, Anthracycline-based Antibody-Drug Conjugates Generated by Enzymatic, Site-specific Conjugation. Mol Cancer Ther. 2017 May;16(5):879-892.