Linker Information

General Information of This Linker
Linker ID
LIN0NFUXE
Linker Name
Mal-PEG4-Val-Ala-PABC
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C33H49N5O11
Isosmiles
CC(NC(=O)C(NC(=O)CCOCCOCCOCCOCCNC(=O)CCN1C(=O)C=CC1=O)C(C)C)C(=O)Nc1ccc(CO)cc1
InChI
InChI=1S/C33H49N5O11/c1-23(2)31(33(45)35-24(3)32(44)36-26-6-4-25(22-39)5-7-26)37-28(41)11-14-46-16-18-48-20-21-49-19-17-47-15-12-34-27(40)10-13-38-29(42)8-9-30(38)43/h4-9,23-24,31,39H,10-22H2,1-3H3,(H,34,40)(H,35,45)(H,36,44)(H,37,41)
InChIKey
JNLGUEGPYJOKEW-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
691.779
Polar area
210.93
Complexity
49
xlogp Value
-0.3493
Heavy Count
49
Rot Bonds
25
Hbond acc
11
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
Mil40-7 [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)
22.00 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)
159.40 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) > 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
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 Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates. Drug Deliv. 2021 Dec;28(1):2603-2617.

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