Payload Information

General Information of This Payload
Payload ID
PAY0PYFPP
Name
PBD dimer 14a
Synonyms
PBD dimer 14a
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Target(s) Human Deoxyribonucleic acid (hDNA)
 Target Info 
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
EGFR-ADC 13a [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) High EGFR expression (EGFR+++)
Method Description
Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC 14a at a single i.v. dose of 3.7 mg/kg.
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) High EGFR expression (EGFR+++)
Method Description
Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC14aat a single i.v. dose of 14.9 mg/kg.
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) High EGFR expression (EGFR+++)
Method Description
Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC14aat a single i.v. dose of 7.4 mg/kg.
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
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)
0.30 nM
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)
3.00 nM
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) > 3.00 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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