Linker Information

General Information of This Linker
Linker ID
LIN0SRKOA
Linker Name
Mal-PEG2-Val-Ala-PABC
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C29H41N5O9
Isosmiles
CC(NC(=O)C(NC(=O)CCOCCOCCNC(=O)CCN1C(=O)C=CC1=O)C(C)C)C(=O)Nc1ccc(CO)cc1
InChI
InChI=1S/C29H41N5O9/c1-19(2)27(29(41)31-20(3)28(40)32-22-6-4-21(18-35)5-7-22)33-24(37)11-14-42-16-17-43-15-12-30-23(36)10-13-34-25(38)8-9-26(34)39/h4-9,19-20,27,35H,10-18H2,1-3H3,(H,30,36)(H,31,41)(H,32,40)(H,33,37)
InChIKey
MDBYVULYLVHMGQ-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
603.673
Polar area
192.47
Complexity
43
xlogp Value
-0.3825
Heavy Count
43
Rot Bonds
19
Hbond acc
9
Hbond Donor
5
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Mil40-6 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
15.90 nM
High HER2 expression (HER2+++)
Method Description
SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model Invasive breast carcinoma BT474 HerDR cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
320.80 nM
High HER2 expression (HER2+++)
Method Description
SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
484.71 nM
Negative HER2 expression (HER2-)
Method Description
SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 nM Negative HER2 expression (HER2-)
Method Description
SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates. Drug Deliv. 2021 Dec;28(1):2603-2617.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.