General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0CBQHP
ADC Name
Anti-KIT 9P3?CX1-1-DM1
Synonyms
Anti-KIT-9P3?CX1-1-DM1
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Organization
Novartis AG
Drug Status
Investigative
Indication
In total 3 Indication(s)
Acute myeloid leukaemia [ICD11:2A60]
Investigative
Melanoma [ICD11:2C30]
Investigative
Small cell lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
3-4
Antibody Name
Anti-KIT mAb 9P3
 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
2,5-Dioxopyrrolidin-1-yl 17-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-5,8,11,14-tetraazaheptadecan-1-oate (CX1-1)
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Max inhibition rate (MIR) 
95
nM
CVCL_2481
Erythroleukemia
Max inhibition rate (MIR) 
55
%
CVCL_7040
Gastrointestinal stromal tumor
Max inhibition rate (MIR) 
100
%
CVCL_0589
Myeloid leukemia with maturation
Max inhibition rate (MIR) 
100
%
CVCL_2196
Adult acute myeloid leukemia
Max inhibition rate (MIR) 
100
%
CVCL_1453
Lung small cell carcinoma
Half Maximum Growth Inhibitory Concentration (GI50) 
0.02
nM
CVCL_0589
Myeloid leukemia with maturation
Half Maximum Growth Inhibitory Concentration (GI50) 
0.04
nM
CVCL_7040
Gastrointestinal stromal tumor
Half Maximum Growth Inhibitory Concentration (GI50) 
1.45
nM
CVCL_1453
Lung small cell carcinoma
Half Maximum Growth Inhibitory Concentration (GI50) 
5.2
nM
CVCL_2196
Adult acute myeloid leukemia
Half Maximum Growth Inhibitory Concentration (GI50) 
7.6
nM
CVCL_2481
Erythroleukemia
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Max inhibition rate (MIR) 95.00 nM Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Erythroleukemia HEL 92.1.7 cells CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Max inhibition rate (MIR) 55.00% Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Gastrointestinal stromal tumor GIST430 cells CVCL_7040
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Max inhibition rate (MIR) 100.00% Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Myeloid leukemia with maturation Kasumi-1 cells CVCL_0589
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Max inhibition rate (MIR) 100.00% Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Adult acute myeloid leukemia SKNO-1 cells CVCL_2196
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Max inhibition rate (MIR) 100.00% Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Lung small cell carcinoma NCI-H1048 cells CVCL_1453
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximum Growth Inhibitory Concentration (GI50) 0.02 nM Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Myeloid leukemia with maturation Kasumi-1 cells CVCL_0589
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximum Growth Inhibitory Concentration (GI50) 0.04 nM Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Gastrointestinal stromal tumor GIST430 cells CVCL_7040
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximum Growth Inhibitory Concentration (GI50) 1.45 nM Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Lung small cell carcinoma NCI-H1048 cells CVCL_1453
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximum Growth Inhibitory Concentration (GI50) 5.20 nM Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Adult acute myeloid leukemia SKNO-1 cells CVCL_2196
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximum Growth Inhibitory Concentration (GI50) 7.60 nM Positive KIT expression (KIT+++/++)
Method Description
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.

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In Vitro Model Erythroleukemia HEL 92.1.7 cells CVCL_2481
References
Ref 1 Antibody drug conjugates.

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