General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XEHSP
ADC Name
ZA202500415A-ADC Example 3
Synonyms
ZA202500415A-ADC Example 3
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Organization
MYRICX PHARMA LIMITED | IMPERIAL COLLEGE INNOVATIONS LIMITED
Drug Status
Investigative
Drug-to-Antibody Ratio
5
Structure
Antibody Name
Sacituzumab
 Antibody Info 
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
 Antigen Info 
Payload Name
NMT inhibitor 1
 Payload Info 
Therapeutic Target
N-Myristoyltransferase (NMT)
 Target Info 
Linker Name
ZA202500415A-ADC-Example-1-Linker
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth lnhibition value (TGl) 
74.76
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
121.55
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
122.04
%
Undisclosed Undisclosed
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.423
uM
CVCL_2962
Gastric adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.486
uM
CVCL_2077
Breast ductal carcinoma
Half Maximal inhibitory Concentration (lC50) 
0.544
uM
CVCL_0455
Lung mucoepidermoid carcinoma
Half Maximal inhibitory Concentration (lC50) 
3.999
uM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
51.61
uM
CVCL_1535
Lung squamous cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
74.76%
Method Description
Cell line-derived xenograft models were established in female NOD/SCID mice, by subcutaneous injection of 5x106 (JIMT-1) tumor cells, and treatmen with 2.5mg/kg ADC (Qw&#422) after tumor volume about 160.66mm3. Determined tumor volume after the experiment, measured at day 27.
In Vivo Model JIMT-1 Breast cancer xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
121.55%
Method Description
Cell line-derived xenograft models were established in female NOD/SCID mice, by subcutaneous injection of 5x106 (JIMT-1) tumor cells, and treatmen with 10mg/kg ADC (Qw&#422) after tumor volume about 160.66mm3. Determined tumor volume after the experiment, measured at day 27.
In Vivo Model JIMT-1 Breast cancer xenograft model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
122.04%
Method Description
Cell line-derived xenograft models were established in female NOD/SCID mice, by subcutaneous injection of 5x106 (JIMT-1) tumor cells, and treatmen with 5mg/kg ADC (Qw&#422) after tumor volume about 160.66mm3. Determined tumor volume after the experiment, measured at day 27.
In Vivo Model JIMT-1 Breast cancer xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.423 uM
Method Description
IM95-m Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Gastric adenocarcinoma IM95-m cells CVCL_2962
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.486 uM Positive her2 expression (her2+++/++)
Method Description
JIMT 1 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.544 uM
Method Description
NCI H292 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 3.999 uM Positive her2 expression (her2+++/++)
Method Description
NCI N87 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
51.61 uM
Method Description
NCI H2170 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Lung squamous cell carcinoma NCI-H2170 cells CVCL_1535
References
Ref 1 Antibody drug conjugate comprising NMT inhibitor and its use