Linker Information

General Information of This Linker
Linker ID
LIN0ZQDJX
Linker Name
N-succinimidyl 3-(2-pyridyldithio) propionate (SPDP)
Linker Type
Flexible dual-reactive (amino/thiol) linker; Thiol-sensitive linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C12H12N2O4S2
Isosmiles
C1CC(=O)N(C1=O)OC(=O)CCSSC2=CC=CC=N2
PubChem CID
100682
InChI
InChI=1S/C12H12N2O4S2/c15-10-4-5-11(16)14(10)18-12(17)6-8-19-20-9-3-1-2-7-13-9/h1-3,7H,4-6,8H2
InChIKey
JWDFQMWEFLOOED-UHFFFAOYSA-N
IUPAC Name
(2,5-dioxopyrrolidin-1-yl) 3-(pyridin-2-yldisulfanyl)propanoate
Pharmaceutical Properties
Molecule Weight
312.4
Polar area
127
Complexity
376
xlogp Value
0.7
Heavy Count
20
Rot Bonds
7
Hbond acc
7
Hbond Donor
0
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Quinoin cetuximab immunoconjugate [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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
27.7 nM
Positive EGFR expression (EGFR +++/++)
Method Description
Cells were treated with different concentrations of drugs for 72 h. The viability was determined using the MTT assay.
In Vitro Model Colon carcinoma GEO cells (Cetuximab-resistant) CVCL_0271
Y-TR1 SPDP [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)
35 ug/mL
Positive CD26 expression (CD26+++/++)
Method Description
Viability assay of Jurkat cells incubated for 72 h with ADC.
In Vitro Model T acute lymphoblastic leukemia Jurkat cells CVCL_0065
T4H11-DM4 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3.35&#1770.53 nM
Positive DDR1 expression (DDR1+++/++)
Method Description
The in vitro cytotoxicity of T4H11 and T4H11-DM4 were evaluated in BC cell lines that expressed different levels of DDR1. The cells were plated at a density of 3.5-5 × 102 cells per 96-well in 100 ul of medium. After overnight incubation, T4H11 and T4H11-DM4 were diluted by consecutive double dilutions and added to different wells. The concentrations of the two drugs ranged from 1.95 to 1000 nM. After 72 h of drug exposure, cell viability was measured by Cell Counting Kit-8 (CCK-8; Dojindo, China) assays. The half-maximal inhibitory concentration (IC50) of the ADC was calculated using GraphPad Prism.

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In Vitro Model Invasive breast carcinoma ZR-75-1 cells CVCL_0588
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
7.44&#1771.18 nM
Positive DDR1 expression (DDR1+++/++)
Method Description
The in vitro cytotoxicity of T4H11 and T4H11-DM4 were evaluated in BC cell lines that expressed different levels of DDR1. The cells were plated at a density of 3.5-5 × 102 cells per 96-well in 100 ul of medium. After overnight incubation, T4H11 and T4H11-DM4 were diluted by consecutive double dilutions and added to different wells. The concentrations of the two drugs ranged from 1.95 to 1000 nM. After 72 h of drug exposure, cell viability was measured by Cell Counting Kit-8 (CCK-8; Dojindo, China) assays. The half-maximal inhibitory concentration (IC50) of the ADC was calculated using GraphPad Prism.

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In Vitro Model Invasive breast carcinoma of no special type T47D cells CVCL_0553
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
13.85&#1772.08 nM
Positive DDR1 expression (DDR1+++/++)
Method Description
The in vitro cytotoxicity of T4H11 and T4H11-DM4 were evaluated in BC cell lines that expressed different levels of DDR1. The cells were plated at a density of 3.5-5 × 102 cells per 96-well in 100 ul of medium. After overnight incubation, T4H11 and T4H11-DM4 were diluted by consecutive double dilutions and added to different wells. The concentrations of the two drugs ranged from 1.95 to 1000 nM. After 72 h of drug exposure, cell viability was measured by Cell Counting Kit-8 (CCK-8; Dojindo, China) assays. The half-maximal inhibitory concentration (IC50) of the ADC was calculated using GraphPad Prism.

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In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
47.49&#1771.14 nM
Positive DDR1 expression (DDR1+++/++)
Method Description
The in vitro cytotoxicity of T4H11 and T4H11-DM4 were evaluated in BC cell lines that expressed different levels of DDR1. The cells were plated at a density of 3.5-5 × 102 cells per 96-well in 100 ul of medium. After overnight incubation, T4H11 and T4H11-DM4 were diluted by consecutive double dilutions and added to different wells. The concentrations of the two drugs ranged from 1.95 to 1000 nM. After 72 h of drug exposure, cell viability was measured by Cell Counting Kit-8 (CCK-8; Dojindo, China) assays. The half-maximal inhibitory concentration (IC50) of the ADC was calculated using GraphPad Prism.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
107.5&#1770.25 nM
Positive DDR1 expression (DDR1+++/++)
Method Description
The in vitro cytotoxicity of T4H11 and T4H11-DM4 were evaluated in BC cell lines that expressed different levels of DDR1. The cells were plated at a density of 3.5-5 × 102 cells per 96-well in 100 ul of medium. After overnight incubation, T4H11 and T4H11-DM4 were diluted by consecutive double dilutions and added to different wells. The concentrations of the two drugs ranged from 1.95 to 1000 nM. After 72 h of drug exposure, cell viability was measured by Cell Counting Kit-8 (CCK-8; Dojindo, China) assays. The half-maximal inhibitory concentration (IC50) of the ADC was calculated using GraphPad Prism.

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In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 6 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM Positive DDR1 expression (DDR1+++/++)
Method Description
The in vitro cytotoxicity of T4H11 and T4H11-DM4 were evaluated in BC cell lines that expressed different levels of DDR1. The cells were plated at a density of 3.5-5 × 102 cells per 96-well in 100 ul of medium. After overnight incubation, T4H11 and T4H11-DM4 were diluted by consecutive double dilutions and added to different wells. The concentrations of the two drugs ranged from 1.95 to 1000 nM. After 72 h of drug exposure, cell viability was measured by Cell Counting Kit-8 (CCK-8; Dojindo, China) assays. The half-maximal inhibitory concentration (IC50) of the ADC was calculated using GraphPad Prism.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 A Novel EGFR Targeted Immunotoxin Based on Cetuximab and Type 1 RIP Quinoin Overcomes the Cetuximab Resistance in Colorectal Cancer Cells. Toxins (Basel). 2023 Jan 9;15(1):57. doi: 10.3390/toxins15010057.
Ref 2 Novel Antibody-Drug Conjugate with Anti-CD26 Humanized Monoclonal Antibody and Transcription Factor IIH (TFIIH) Inhibitor, Triptolide, Inhibits Tumor Growth via Impairing mRNA Synthesis. Cancers (Basel). 2019 Aug 8;11(8):1138. doi: 10.3390/cancers11081138.
Ref 3 Antibody-drug conjugates targeting DDR1 as a novel strategy for treatment of breast cancer