Payload Information
General Information of This Payload
| Payload ID | PAY0RMJYN |
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| Name | 6i-5657 Payload |
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| Synonyms |
6i-5657 Payload
Click to Show/Hide
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| Target | DNA topoisomerase I (TOP1) | |||||
| Structure |
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| Formula | C26H26FN3O4 |
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| Isosmiles | CN([C@H](C1=C2CN3C(C(COC4=O)=C([C@@]4(O)CC)C=C3C2=NC5=C16)=O)CCC6=C(C(F)=C5)C)C |
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| PubChem CID | ||||||
| InChI |
InChI=1S/C26H26FN3O4/c1-5-26(33)16-8-20-23-14(10-30(20)24(31)15(16)11-34-25(26)32)22-19(29(3)4)7-6-13-12(2)17(27)9-18(28-23)21(13)22/h8-9,19,33H,5-7,10-11H2,1-4H3/t19-,26-/m0/s1
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| InChIKey |
PJLABXDCBXXRNW-SIBVEZHUSA-N
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| Pharmaceutical Properties | Molecule Weight |
463.509 |
Polar area |
84.66 |
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Complexity |
1454.352438 |
xlogp Value |
3.07602 |
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Heavy Count |
34 |
Rot Bonds |
2 |
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Hbond acc |
7 |
Hbond Donor |
1 |
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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
wO2024105206A1 5k-2658 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
1.0- 9.9 nM
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| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 14 % carbon dioxide.
Click to Show/Hide
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| In Vitro Model | Renal cell carcinoma | 786-O cells (+NE) | CVCL_1051 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
10- 99 nM
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| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 14 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Renal cell carcinoma | 786-O cells (-NE) | CVCL_1051 | ||
wO2024105206A1 6i-5657 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
1.0- 9.9 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Renal cell carcinoma | 786-O cells (+NE) | CVCL_1051 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
10- 99 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Renal cell carcinoma | 786-O cells (-NE) | CVCL_1051 | ||
wO2024105206A1 6k-2658 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
1.0- 9.9 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 16 % carbon dioxide.
Click to Show/Hide
|
||||
| In Vitro Model | Renal cell carcinoma | 786-O cells (+NE) | CVCL_1051 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Activity Concentration at -50% (AC50) |
10- 99 nM
|
|||
| Method Description |
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 16 % carbon dioxide.
Click to Show/Hide
|
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| In Vitro Model | Renal cell carcinoma | 786-O cells (-NE) | CVCL_1051 | ||
