Linker Information

General Information of This Linker
Linker ID
LIN0LBSCH
Linker Name
BIMPRO
Linker Type
Flexible dual-reactive (amino/thiol) linker
Antibody-Linker Relation
Uncleavable
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
THL4-mpeoDM1 [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 51.61% (Day 24) Positive DLL4 expression (DLL4 +++/++)
Method Description
Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 1.5 mg/kg HLmD4 was intravenously administered once every three days for three weeks.
In Vivo Model A549 CDX model
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 57.73% (Day 24) Positive DLL4 expression (DLL4 +++/++)
Method Description
Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 1.5 mg/kg HLmD4 was intravenously administered once every three days for three weeks.
In Vivo Model MDA-MB-231 CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.25% (Day 24) Positive DLL4 expression (DLL4 +++/++)
Method Description
Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg HLmD4 was intravenously administered once every three days for three weeks.
In Vivo Model A549 CDX model
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.11% (Day 24) Positive DLL4 expression (DLL4 +++/++)
Method Description
Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg HLmD4 was intravenously administered once every three days for three weeks.
In Vivo Model MDA-MB-231 CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
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)
37.45 nM
Positive DLL4 expression (DLL4 +++/++)
Method Description
In vitro cytotoxicity and mechanism of anti-DLL4 ADCs. The cytotoxicity of ADCs was assessed by MTT assay. The percentage of cell inhibition relative to untreated control HUVEC cells was calculated for each drug concentration.
In Vitro Model Normal HUVEC-C cells CVCL_2959
H3L2-mpeoDM1 [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.38% (Day 24) Positive DLL4 expression (DLL4 +++/++)
Method Description
Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg JmD4 was intravenously administered once every three days for three weeks.
In Vivo Model A549 CDX model
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88.43% (Day 24) Positive DLL4 expression (DLL4 +++/++)
Method Description
Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg JmD4 was intravenously administered once every three days for three weeks.
In Vivo Model MDA-MB-231 CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
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)
36.12 nM
Positive DLL4 expression (DLL4 +++/++)
Method Description
In vitro cytotoxicity and mechanism of anti-DLL4 ADCs. The cytotoxicity of ADCs was assessed by MTT assay. The percentage of cell inhibition relative to untreated control HUVEC cells was calculated for each drug concentration.
In Vitro Model Normal HUVEC-C cells CVCL_2959
References
Ref 1 Two engineered site-specific antibody-drug conjugates, HLmD4 and HLvM4, have potent therapeutic activity in two DLL4-positive tumour xenograft models. Am J Cancer Res. 2020 Aug 1;10(8):2387-2408. eCollection 2020.

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