General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0RQKHA
ADC Name
NN2101-DM1
Synonyms
NN2101 DM1
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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
Click To Hide/Show 9 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 2.01
%
HMC-1.2 cells
Mast cell leukemia
Tumor Growth Inhibition value (TGI) 
≈ 12.3
%
GIST-T1 cells
Gastrointestinal stromal tumor
Tumor Growth Inhibition value (TGI) 
≈ 20.5
%
NCI-H526 cells
Lung small cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 50.4
%
Huh-7 cells
Adult hepatocellular carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 61.3
%
HMC-1.2 cells
Mast cell leukemia
Tumor Growth Inhibition value (TGI) 
≈ 61.3
%
HMC-1.2 cells
Mast cell leukemia
Tumor Growth Inhibition value (TGI) 
≈ 87.9
%
Huh-7 cells
Adult hepatocellular carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 90.1
%
GIST-T1 cells
Gastrointestinal stromal tumor
Tumor Growth Inhibition value (TGI) 
≈ 94.3
%
NCI-H526 cells
Lung small cell carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 19 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.38
ng/mL
GIST-T1 cells
Gastrointestinal stromal tumor
Half Maximal Inhibitory Concentration (IC50) 
0.43
ng/mL
GIST-430/654 cells
Gastrointestinal stromal tumor
Half Maximal Inhibitory Concentration (IC50) 
2.02
ng/mL
GIST430 cells
Gastrointestinal stromal tumor
Half Maximal Inhibitory Concentration (IC50) 
8.07
ng/mL
NCI-H526 cells
Lung small cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.77
ug/mL
HMC-1.2 cells
Mast cell leukemia
Half Maximal Inhibitory Concentration (IC50) 
1.18
ug/mL
NCI-H1048 cells
Lung small cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
2.52
ug/mL
Caov-3 cells
Ovarian serous adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
2.54
ug/mL
MDA-MB-468 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
2.99
ug/mL
MDA-MB-453 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
3.71
ug/mL
NCI-H2170 cells
Lung squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
4.03
ug/mL
OVCAR-3 cells
Ovarian serous adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
4.3
ug/mL
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
5.47
ug/mL
Kasumi-1 cells
Myeloid leukemia with maturation
Half Maximal Inhibitory Concentration (IC50) 
7.38
ug/mL
TF-1 cells
Esophageal squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
11.84
ug/mL
COS-7 cells
Normal
Half Maximal Inhibitory Concentration (IC50) 
11.95
ug/mL
HUVEC-C cells
Normal
Half Maximal Inhibitory Concentration (IC50) 
12.47
ug/mL
NCI-H889 cells
Lung small cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
17.49
ug/mL
GIST48 cells
Gastrointestinal stromal tumor
Half Maximal Inhibitory Concentration (IC50) 
17.63
ug/mL
Ms-1 cells
Lung small cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
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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