Antibody Information

General Information of This Antibody
Antibody ID
ANI0UQBLV
Antibody Name
NN2101
Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized IgG1-kappa
Antigen Name
Mast/stem cell growth factor receptor Kit (KIT)
  Antigen Info 
Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
NN2101-DM1 [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 9 Activity Data Related to This Level
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.

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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.

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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.

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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.

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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.

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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.

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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).

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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).

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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
Click To Hide/Show 19 Activity Data Related to This Level
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
Ref 1 A novel anti-c-Kit antibody-drug conjugate to treat wild-type and activating-mutant c-Kit-positive tumors. Mol Oncol. 2022 Mar;16(6):1290-1308.

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