General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XCOMM
ADC Name
T4H11-DM4
Synonyms
T4H11-DM4
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Organization
Sichuan University.; West China Hospital of Sichuan University.
Drug Status
Investigative
Structure
Antibody Name
T4H11
 Antibody Info 
Antigen Name
Epithelial discoidin domain-containing receptor 1 (DDR1)
 Antigen Info 
Payload Name
Mertansine DM4
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
N-succinimidyl 3- (2-pyridyldithio) propionate (SPDP)
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
3.35&#1770.53
nM
CVCL_0588
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
7.44&#1771.18
nM
CVCL_0553
Invasive breast carcinoma of no special type
Half Maximal inhibitory Concentration (lC50) 
13.85&#1772.08
nM
CVCL_0179
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
47.49&#1771.14
nM
CVCL_0033
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
107.5&#1770.25
nM
CVCL_0062
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
> 1000
nM
CVCL_0031
Invasive breast carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
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 [1]
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 [1]
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 [1]
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 [1]
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 [1]
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 [1]
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 Antibody-drug conjugates targeting DDR1 as a novel strategy for treatment of breast cancer