Linker Information

General Information of This Linker
Linker ID
LIN0SMWAK
Linker Name
Hexapeptide linker ASTKGP
Linker Type
Lysine-based site-specific conjugation linker
Antibody-Linker Relation
Uncleavable
Structure
Formula
C28H40N4O8
Isosmiles
CC(C)C(C(=O)O)N(C)C(=O)CCCCCNC(=O)COCC(=O)Nc1ccc(CCC(=O)N2CCC2=O)cc1
InChI
InChI=1S/C28H40N4O8/c1-19(2)27(28(38)39)31(3)24(35)7-5-4-6-15-29-22(33)17-40-18-23(34)30-21-11-8-20(9-12-21)10-13-25(36)32-16-14-26(32)37/h8-9,11-12,19,27H,4-7,10,13-18H2,1-3H3,(H,29,33)(H,30,34)(H,38,39)
InChIKey
ZFRVGWNMJONSGC-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
560.648
Polar area
162.42
Complexity
40
xlogp Value
1.5774
Heavy Count
40
Rot Bonds
17
Hbond acc
7
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Trastuzumab DVD-ADC [Investigative]
 ADC Info 
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 Inhibition rate (100nM)
0.00%
High TRKB expression (TRKB+++); Negative HER2 expression (HER2-)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Inhibition rate (100nM)
0.00%
High TRKB expression (TRKB+++); Negative HER2 expression (HER2-)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Inhibition rate (100nM) > 50.00% High HER2 expression (HER2+++); Moderate TRKB expression (TRKB++)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
References
Ref 1 A new immunochemical strategy for triple-negative breast cancer therapy. Sci Rep. 2021 Jul 21;11(1):14875.

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