Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0UDBKJ
ADC Name
EGFR-ADC 13b
Synonyms
EGFR ADC 13b
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Squamous cell cancer [ICD11:2D60-2D61]
Investigative
Drug-to-Antibody Ratio
3.2
Antibody Name
Anti-EGFR mAb
  Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
  Antigen Info 
Payload Name
PBD dimer 14b
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Adipic acid-Val-Ala-PABC
  Linker Info 
Conjugate Type
Random conjugation through nucleophilic lysines.
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
6
pM
HSC-2 cells
Oral cavity squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
30
pM
KB cells
Human papillomavirus-related endocervical adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.3
nM
NCI-H2110 cells
Lung non-small cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 6.00 pM Positive EGFR expression (EGFR+++/++)
Method Description
Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model Oral cavity squamous cell carcinoma HSC-2 cells CVCL_1287
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 30.00 pM Positive EGFR expression (EGFR+++/++)
Method Description
Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.30 nM Negative EGFR expression (EGFR-)
Method Description
Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model Lung non-small cell carcinoma NCI-H2110 cells CVCL_1530
References
Ref 1 Synthesis of Highly Potent N-10 Amino-Linked DNA-Alkylating Indolinobenzodiazepine Antibody-Drug Conjugates (ADCs). ACS Med Chem Lett. 2019 Jul 22;10(8):1211-1215. doi: 10.1021/acsmedchemlett.9b00254. eCollection 2019 Aug 8.

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