Linker Information

General Information of This Linker

Linker ID	LIN0NBUDP
Linker Name	AJICAP
Linker Type	Peptide-based site-specific conjugation linker
Antibody-Linker Relation	Uncleavable
Structure
Structure	3D MOL		2D MOL
Formula	C19H23N3O7S
Isosmiles	NC(=O)CCSC1=CC(=O)N(CC2CCC(C(=O)ON3C(=O)CCC3=O)CC2)C1=O
InChI	InChI=1S/C19H23N3O7S/c20-14(23)7-8-30-13-9-17(26)21(18(13)27)10-11-1-3-12(4-2-11)19(28)29-22-15(24)5-6-16(22)25/h9,11-12H,1-8,10H2,(H2,20,23)
InChIKey	BSYHAJOCHZXFFP-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	437.474	Polar area	144.15
	Complexity	30	xlogp Value	0.2613
	Heavy Count	30	Rot Bonds	8
	Hbond acc	8	Hbond Donor	1

Each Antibody-drug Conjugate Related to This Linker

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

Trastuzumab-AJICAP-maytansinoid [Investigative]

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	Minimal Effective Dose (MED)	< 5.00 mg/kg	High HER2 expression (HER2+++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: three trastuzumab-AJICAP-maytansinoid groups, treated with 20 mg/kg, 60 mg/kg, and 120 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements. Click to Show/Hide
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Maximum Tolerated Dose (MTD)	> 120.00 mg/kg	High HER2 expression (HER2+++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: three trastuzumab-AJICAP-maytansinoid groups, treated with 20 mg/kg, 60 mg/kg, and 120 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements. Click to Show/Hide
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

References

Ref 1	Biological Evaluation of Maytansinoid-Based Site-Specific Antibody-Drug Conjugate Produced by Fully Chemical Conjugation Approach: AJICAP. Front Biosci (Landmark Ed). 2022 Aug 5;27(8):234.