General Information of This Payload
Payload ID
PAY0WTZYO
Name
NMT inhibitor 1
Synonyms
NMT inhibitor 1
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Target N-Myristoyltransferase (NMT)
Structure
Formula
C27H33F2N5O2
Isosmiles
CN1C(C)=C(CCOC2=C(F)C(F)=CC=C2C3=CN4C(CNC)=CN=C4C=C3)C(C(O)C(C)(C)C)=N1
PubChem CID
171065696
InChI
InChI=1S/C27H33F2N5O2/c1-16-19(24(32-33(16)6)26(35)27(2,3)4)11-12-36-25-20(8-9-21(28)23(25)29)17-7-10-22-31-14-18(13-30-5)34(22)15-17/h7-10,14-15,26,30,35H,11-13H2,1-6H3
InChIKey
BXIHXITXQCGGOW-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
497.59
Polar area
76.61
Complexity
1345.185515
xlogp Value
4.74182
Heavy Count
36
Rot Bonds
8
Hbond acc
7
Hbond Donor
2
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
ZA202500415A-ADC Example 1 [Investigative]
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.

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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.

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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.

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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.

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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.

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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
ZA202500415A-ADC Example 3 [Investigative]
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
ZA202500415A-ADC Example 4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
104.40%
Method Description
Cell line-derived xenograft models were established in male NOD SCID mice, by subcutaneous injection of 1x107 (LNCaP) tumor cells, and treatmen with 5mg/kg ADC (Q7D&#423) after tumor volume about 80-100mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model LNCaP prostate cancer xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
108.31%
Method Description
Cell line-derived xenograft models were established in non-castrated male CB17/SCID mice, by subcutaneous injection of 1x107 (VCaP) tumor cells, and treatmen with 2.5mg/kg ADC (QW&#422) after tumor volume about 162.16mm3. Determined tumor volume after the experiment, measured at day 17.
In Vivo Model VCaP prostate cancer xenograft model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
112.40%
Method Description
Cell line-derived xenograft models were established in male NOD SCID mice, by subcutaneous injection of 1x107 (LNCaP) tumor cells, and treatmen with 10mg/kg ADC (Q7D&#423) after tumor volume about 80-100mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model LNCaP prostate cancer xenograft model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
114.03%
Method Description
Cell line-derived xenograft models were established in non-castrated male CB17/SCID mice, by subcutaneous injection of 1x107 (VCaP) tumor cells, and treatmen with 10mg/kg ADC (QW&#422) after tumor volume about 162.16mm3. Determined tumor volume after the experiment, measured at day 17.
In Vivo Model VCaP prostate cancer xenograft model
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
114.69%
Method Description
Cell line-derived xenograft models were established in non-castrated male CB17/SCID mice, by subcutaneous injection of 1x107 (VCaP) tumor cells, and treatmen with 5mg/kg ADC (QW&#422) after tumor volume about 162.16mm3. Determined tumor volume after the experiment, measured at day 17.
In Vivo Model VCaP prostate cancer xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.154 uM
Method Description
LNCaP 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 Prostate carcinoma LNCaP cells CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.158 uM
Method Description
VCaP 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 2.2 Solution Cell Viability Assay.

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In Vitro Model Prostate carcinoma VCaP cells CVCL_2235
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.345 uM
Method Description
C42 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 2.1 Solution Cell Viability Assay.

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In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
References
Ref 1 Antibody drug conjugate comprising NMT inhibitor and its use