General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ECRQZ
ADC Name
ZA202500415A-ADC Example 1
Synonyms
ZA202500415A-ADC Example 1
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Organization
MYRICX PHARMA LIMITED | IMPERIAL COLLEGE INNOVATIONS LIMITED
Drug Status
Investigative
Drug-to-Antibody Ratio
5
Structure
Antibody Name
Trastuzumab
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 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 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth lnhibition value (TGl) 
55
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
109
%
Undisclosed Undisclosed
Revealed Based on the Cell Line Data
Click To Hide/Show 23 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.0004
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0005
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0007
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0008
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0022
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0029
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0037
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0044
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0046
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0068
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0093
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0187
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.0226
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
> 0.05
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
> 0.05
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
> 0.05
uM
Undisclosed
Gastric cancer
Half Maximal inhibitory Concentration (lC50) 
0.172
uM
CVCL_0179
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
< 0.2
uM
CVCL_1661
Breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
0.791
uM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
1.581
uM
CVCL_1535
Lung squamous cell carcinoma
Half Maximal inhibitory Concentration (lC50) 
52.07
uM
CVCL_2077
Breast ductal carcinoma
Half Maximal inhibitory Concentration (lC50) 
153.55
uM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
224.01
uM
CVCL_1603
Gastric tubular adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 55% Positive her2 expression (her2+++/++)
Method Description
NOD/SCID mice were implanted with estrogen pellets (17p-estradiol, 60 day release, 0.36mg) subcutaneously in the right flank one day before the tumour inoculation.On day -8 each mouse was then inoculated in the right mammary fat pad with 1x107 (BT474) tumor cells,and treatment with 2.5mpk ADC (once per week for four weeks)after tumor volume about 149.78mm3. Determined tumor volume after the experiment, measured at day 23.

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In Vivo Model BT474 xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 109% Positive her2 expression (her2+++/++)
Method Description
NOD/SCID mice were implanted with estrogen pellets (17p-estradiol, 60 day release, 0.36mg) subcutaneously in the right flank one day before the tumour inoculation.On day -8 each mouse was then inoculated in the right mammary fat pad with 1x107 (BT474) tumor cells,and treatment with 5mpk ADC (once per week for four weeks)after tumor volume about 149.78mm3. Determined tumor volume after the experiment, measured at day 23.

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In Vivo Model BT474 xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 23 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0004 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

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In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0005 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

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In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0007 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0008 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

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In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0022 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

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In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0029 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0037 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0044 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

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In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0046 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0068 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0093 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0187 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.0226 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 0.05 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 15 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 0.05 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 16 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 0.05 uM
Method Description
Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.

   Click to Show/Hide
In Vitro Model Gastric cancer Patient derived gastric cancer cells Homo sapiens
Experiment 17 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.172 uM Positive her2 expression (her2+++/++)
Method Description
BT-474 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 Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 18 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.2 uM
Method Description
ZR-75-30 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 carcinoma ZR-75-30 cells CVCL_1661
Experiment 19 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.791 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 20 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.581 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
Experiment 21 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 52.07 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 22 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 153.55 uM Positive her2 expression (her2+++/++)
Method Description
Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 1x107 (NCI-N87) tumor cells, and treatment with 2.5mg/kg (QW&#422) ADC after tumor volume about 168.08mm3. Determined tumor volume after the experiment, measured at day 35.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 23 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 224.01 uM Positive her2 expression (her2+++/++)
Method Description
Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 1x107 (NCI-N87) tumor cells, and treatment with 5mg/kg (QW&#422) ADC after tumor volume about 168.08mm3. Determined tumor volume after the experiment, measured at day 35.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
References
Ref 1 Antibody drug conjugate comprising NMT inhibitor and its use