General Information of This Linker
Linker ID
LIN0KYSKB
Linker Name
Adipic acid-Val-Ala-PABC
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
EGFR-ADC 13a [Investigative]
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
EGFR-ADC 13c [Investigative]
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)
40.00 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)
0.10 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
EGFR-ADC 13b [Investigative]
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
FOLR1-ADC 13b [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 pM
Positive FOLR1 expression (FOLR1+++/++)
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 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM
Negative FOLR1 expression (FOLR1-)
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 Invasive breast carcinoma T-47D cells CVCL_0553
FOLR1-ADC 13c [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
20.00 pM
Positive FOLR1 expression (FOLR1+++/++)
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 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 nM
Negative FOLR1 expression (FOLR1-)
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 Invasive breast carcinoma T-47D cells CVCL_0553
FOLR1-ADC 13a [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM
Positive FOLR1 expression (FOLR1+++/++)
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 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 3.00 nM Negative FOLR1 expression (FOLR1-)
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 Invasive breast carcinoma T-47D cells CVCL_0553
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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