Linker Information

General Information of This Linker

Linker ID	LIN0NRGVE
Linker Name	PY-VC-PABC
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
Structure	3D MOL		2D MOL
Formula	C32H46N8O8S
Isosmiles	C=CC(=O)N1CN(C(=O)C=C)CN(C(=O)CCSCC(=O)NC(C(=O)NC(CCCNC(N)=O)C(=O)Nc2ccc(CO)cc2)C(C)C)C1
InChI	InChI=1S/C32H46N8O8S/c1-5-26(43)38-18-39(27(44)6-2)20-40(19-38)28(45)13-15-49-17-25(42)37-29(21(3)4)31(47)36-24(8-7-14-34-32(33)48)30(46)35-23-11-9-22(16-41)10-12-23/h5-6,9-12,21,24,29,41H,1-2,7-8,13-20H2,3-4H3,(H,35,46)(H,36,47)(H,37,42)(H3,33,34,48)
InChIKey	HQIKSJQCJBQAKX-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	702.835	Polar area	223.58
	Complexity	49	xlogp Value	0.0587
	Heavy Count	49	Rot Bonds	18
	Hbond acc	9	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

Zapadcine-1 [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 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)	Positive DR5 expression (DR5+++/++)
Method Description	Zapadcine-1 (9 mg/kg, Q3D3, every three days for 3 times) induces efficient tumor cell killing in cell line-derived models of Jurkat E6-1 cells with DR5 expression with high expression.
In Vivo Model	Jurkat E6.1 CDX model
In Vitro Model	Leukemia	Jurkat E6.1 cells		CVCL_0367

RGCLN18.2-PY-Val-Cit-PAB-MMAE [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 Inhibitory Concentration (IC50)	6.23 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

References

Ref 1	A novel anti-DR5 antibody-drug conjugate possesses a high-potential therapeutic efficacy for leukemia and solid tumors. Theranostics. 2019 Jul 13;9(18):5412-5423. doi: 10.7150/thno.33598. eCollection 2019.
Ref 2	Anti-claudin 18.2 antibody and antibody-drug conjugate thereof; 2022-11-17.