Linker Information
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
| 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
| 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
| 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
| 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
| 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
| 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
| 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
If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.
