Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
ADC ID |
DRG0RQKHA
|
|||||
---|---|---|---|---|---|---|
ADC Name |
NN2101-DM1
|
|||||
Synonyms |
NN2101 DM1
Click to Show/Hide
|
|||||
Drug Status |
Investigative
|
|||||
Indication |
In total 5 Indication(s)
Acute myeloid leukaemia [ICD11:2A60]
Investigative
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastrointestinal interstitial cancer [ICD11:2B5B]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
Small cell lung cancer [ICD11:2C25]
Investigative
|
|||||
Drug-to-Antibody Ratio |
1.51
|
|||||
Structure | ||||||
Antibody Name |
NN2101
|
Antibody Info | ||||
Antigen Name |
Mast/stem cell growth factor receptor Kit (KIT)
|
Antigen Info | ||||
Payload Name |
Mertansine DM1
|
Payload Info | ||||
Therapeutic Target |
Microtubule (MT)
|
Target Info | ||||
Linker Name |
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
|
Linker Info | ||||
Conjugate Type |
Random conjugation through nucleophilic lysines.
|
|||||
Combination Type |
Emtansine
|
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 2.01% (Day 20) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,2 mg/kg.
Click to Show/Hide
|
||||
In Vivo Model | GIST xenograft model | ||||
In Vitro Model | Mast cell leukemia | HMC-1.2 cells | CVCL_H205 | ||
Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 12.30% (Day 50) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,1 mg/kg.
Click to Show/Hide
|
||||
In Vivo Model | GIST xenograft model | ||||
In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 20.50% (Day 27) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg.
Click to Show/Hide
|
||||
In Vivo Model | SCLC xenograft model | ||||
In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 50.40% (Day 50) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,1 mg/kg.
Click to Show/Hide
|
||||
In Vivo Model | GIST xenograft model | ||||
In Vitro Model | Adult hepatocellular carcinoma | Huh-7 cells | CVCL_0336 | ||
Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 61.30% (Day 60) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3.5 mg/kg.
Click to Show/Hide
|
||||
In Vivo Model | GIST xenograft model | ||||
In Vitro Model | Mast cell leukemia | HMC-1.2 cells | CVCL_H205 | ||
Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 61.30% (Day 60) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,5 mg/kg.
Click to Show/Hide
|
||||
In Vivo Model | GIST xenograft model | ||||
In Vitro Model | Mast cell leukemia | HMC-1.2 cells | CVCL_H205 | ||
Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 87.90% (Day 50) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg.
Click to Show/Hide
|
||||
In Vivo Model | GIST xenograft model | ||||
In Vitro Model | Adult hepatocellular carcinoma | Huh-7 cells | CVCL_0336 | ||
Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.10% (Day 50) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg. The mice were intraperitoneally administered Etoposide was prepared in dimethyl sulfoxide, and the solution was diluted in PBS just before administration. The mice were intraperitoneally administered etoposide for 2 cycles (3 mg/kg per day;days 15 and days 1115).
Click to Show/Hide
|
||||
In Vivo Model | GIST xenograft model | ||||
In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.30% (Day 27) | Positive KIT expression (KIT+++/++) | ||
Method Description |
The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg. The mice were intraperitoneally administered Etoposide was prepared in dimethyl sulfoxide, and the solution was diluted in PBS just before administration. The mice were intraperitoneally administered etoposide for 2 cycles (3 mg/kg per day;days 15 and days 1115).
Click to Show/Hide
|
||||
In Vivo Model | SCLC xenograft model | ||||
In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.38 ng/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.43 ng/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Gastrointestinal stromal tumor | GIST-430/654 cells | CVCL_7040 | ||
Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2.02 ng/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Gastrointestinal stromal tumor | GIST430 cells | CVCL_7040 | ||
Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 8.07 ng/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.77 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Mast cell leukemia | HMC-1.2 cells | CVCL_H205 | ||
Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.18 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Lung small cell carcinoma | NCI-H1048 cells | CVCL_1453 | ||
Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2.52 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Ovarian serous adenocarcinoma | Caov-3 cells | CVCL_0201 | ||
Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2.54 ug/mL | Negative KIT expression (KIT-) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2.99 ug/mL | Negative KIT expression (KIT-) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 3.71 ug/mL | Negative KIT expression (KIT-) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Lung squamous cell carcinoma | NCI-H2170 cells | CVCL_1535 | ||
Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 4.03 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Ovarian serous adenocarcinoma | OVCAR-3 cells | CVCL_0465 | ||
Experiment 12 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 4.30 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 13 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 5.47 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Myeloid leukemia with maturation | Kasumi-1 cells | CVCL_0589 | ||
Experiment 14 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 7.38 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Esophageal squamous cell carcinoma | TF-1 cells | CVCL_1759 | ||
Experiment 15 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 11.84 ug/mL | Negative KIT expression (KIT-) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Normal | COS-7 cells | CVCL_0224 | ||
Experiment 16 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 11.95 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Normal | HUVEC-C cells | CVCL_2959 | ||
Experiment 17 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 12.47 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Lung small cell carcinoma | NCI-H889 cells | CVCL_1598 | ||
Experiment 18 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 17.49 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Gastrointestinal stromal tumor | GIST48 cells | CVCL_7041 | ||
Experiment 19 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 17.63 ug/mL | Positive KIT expression (KIT+++/++) | ||
Method Description |
For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
|
||||
In Vitro Model | Lung small cell carcinoma | Ms-1 cells | CVCL_IQ55 |
References
If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.