Payload Information
General Information of This Payload
| Payload ID | PAY0EKLMT |
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|---|---|---|---|---|---|---|
| Name | Exatecan-Gly amide |
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| Synonyms |
compound 10
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| Target | DNA topoisomerase I (TOP1) | |||||
| Structure |
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| Formula | C24H23FN4O5 |
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| Isosmiles | O=C(NC1=C(F)C=C2N=C3C(CN4C(C(COC([C@@]5(CC)O)=O)=C5C=C43)=O)=C(CC)C2=C1)CN |
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| InChI |
InChI=1S/C24H23FN4O5/c1-3-11-12-5-18(27-20(30)8-26)16(25)7-17(12)28-21-13(11)9-29-19(21)6-15-14(22(29)31)10-34-23(32)24(15,33)4-2/h5-7,33H,3-4,8-10,26H2,1-2H3,(H,27,30)/t24-/m0/s1
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| InChIKey |
SFYJSYKEMCZJCX-DEOSSOPVSA-N
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| Pharmaceutical Properties | Molecule Weight |
466.469 |
Polar area |
136.54 |
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Complexity |
1421.139497 |
xlogp Value |
1.6783 |
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Heavy Count |
34 |
Rot Bonds |
4 |
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Hbond acc |
8 |
Hbond Donor |
3 |
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Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
wO2024239281A1 C144 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.011 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
C4-2B is both Steap1 and PSMA antigen high express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
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| In Vitro Model | Prostate carcinoma | C4-2B cells | CVCL_4784 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.012 nM
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High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
PC-3-4H7 cell is both Steap1and PSMA antigen high express cells. To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
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|
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| In Vitro Model | Prostate carcinoma | PC-3-4H7 cells | Homo sapiens | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
4.28 nM
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Low Steap1 and PSMA expression (Steap1 and PSMA+) | ||
| Method Description |
22RV1 is both Steapl and PSMA antigen low express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
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| In Vitro Model | Prostate carcinoma | 22RV1 cells | CVCL_1045 | ||
wO2024239281A1 C158 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.019 nM
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High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
PC-3-4H7 cell is both Steap1and PSMA antigen high express cells. To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
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| In Vitro Model | Prostate carcinoma | PC-3-4H7 cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.025 nM
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High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
C4-2B is both Steap1 and PSMA antigen high express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | C4-2B cells | CVCL_4784 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
6.12 nM
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Low Steap1 and PSMA expression (Steap1 and PSMA+) | ||
| Method Description |
22RV1 is both Steapl and PSMA antigen low express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
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| In Vitro Model | Prostate carcinoma | 22RV1 cells | CVCL_1045 | ||
wO2024239281A1 C112 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.039 nM
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High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
PC-3-4H7 cell is both Steap1and PSMA antigen high express cells. To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | PC-3-4H7 cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.047 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
C4-2B is both Steap1 and PSMA antigen high express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | C4-2B cells | CVCL_4784 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
8.28 nM
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Low Steap1 and PSMA expression (Steap1 and PSMA+) | ||
| Method Description |
22RV1 is both Steapl and PSMA antigen low express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | 22RV1 cells | CVCL_1045 | ||
wO2024239281A1 C031 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.052 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
PC-3-4H7 cell is both Steap1 and PSMA antigen high express cells. To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | PC-3-4H7 cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.064 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
C4-2B is both Steap1 and PSMA antigen high express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | C4-2B cells | CVCL_4784 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
9.72 nM
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Low Steap1 and PSMA expression (Steap1 and PSMA+) | ||
| Method Description |
22RV1 is both Steapl and PSMA antigen low express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | 22RV1 cells | CVCL_1045 | ||
wO2024239281A1 C039 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.053 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
PC-3-4H7 cell is both Steap1and PSMA antigen high express cells. To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | PC-3-4H7 cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.062 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
C4-2B is both Steap1 and PSMA antigen high express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | C4-2B cells | CVCL_4784 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
8.95 nM
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Low Steap1 and PSMA expression (Steap1 and PSMA+) | ||
| Method Description |
22RV1 is both Steapl and PSMA antigen low express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | 22RV1 cells | CVCL_1045 | ||
wO2024239281A1 C084C [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.075 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
C4-2B is both Steap1 and PSMA antigen high express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | C4-2B cells | CVCL_4784 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.093 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
PC-3-4H7 cell is both Steap1and PSMA antigen high express cells. To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | PC-3-4H7 cells | Homo sapiens | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
11.7 nM
|
Low Steap1 and PSMA expression (Steap1 and PSMA+) | ||
| Method Description |
22RV1 is both Steapl and PSMA antigen low express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | 22RV1 cells | CVCL_1045 | ||
wO2024239281A1 C084 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.078 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
C4-2B is both Steap1 and PSMA antigen high express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | C4-2B cells | CVCL_4784 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.095 nM
|
High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
PC-3-4H7 cell is both Steap1and PSMA antigen high express cells. To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | PC-3-4H7 cells | Homo sapiens | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
10.5 nM
|
Low Steap1 and PSMA expression (Steap1 and PSMA+) | ||
| Method Description |
22RV1 is both Steapl and PSMA antigen low express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
Click to Show/Hide
|
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| In Vitro Model | Prostate carcinoma | 22RV1 cells | CVCL_1045 | ||
References