Payload Information
General Information of This Payload
| Payload ID | PAY0RPNAQ |
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|---|---|---|---|---|---|---|
| Name | Methylenedioxy CPT1 (CPT1) |
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| Synonyms |
Methylenedioxy CPT1 (CPT1)
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| Target(s) | DNA topoisomerase 1 (TOP1) | |||||
| Structure |
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| Formula | C22H19N3O6 |
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| Isosmiles | CCC1(O)C(=O)OCc2c1cc1n(c2=O)Cc2c-1nc1cc3c(cc1c2CN)OCO3 |
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| InChI |
InChI=1S/C22H19N3O6/c1-2-22(28)14-4-16-19-12(7-25(16)20(26)13(14)8-29-21(22)27)11(6-23)10-3-17-18(31-9-30-17)5-15(10)24-19/h3-5,28H,2,6-9,23H2,1H3
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| InChIKey |
QILNNZJGRYNYJV-UHFFFAOYSA-N
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| Pharmaceutical Properties | Molecule Weight |
421.409 |
Polar area |
125.9 |
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Complexity |
31 |
xlogp Value |
1.267 |
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Heavy Count |
31 |
Rot Bonds |
2 |
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Hbond acc |
9 |
Hbond Donor |
2 |
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The activity data of This Payload
| Standard Type | Value | Units | Cell line | Disease Model | Cell line ID | Reference |
|---|---|---|---|---|---|---|
| Half Maximal Inhibitory Concentration (IC50) | 0.7 | nmol/L |
DEL cells
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Anaplastic large cell lymphoma
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[1] | |
| Half Maximal Inhibitory Concentration (IC50) | 1 | nmol/L |
L540cy cells
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Hodgkin's disease
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Undisclosed | [1] |
| Half Maximal Inhibitory Concentration (IC50) | 1 | nmol/L |
DEL/BVR cells
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Anaplastic large cell lymphoma
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[1] | |
| Half Maximal Inhibitory Concentration (IC50) | 2 | nmol/L |
Karpas-299 cells
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ALK-positive anaplastic large cell lymphoma
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[1] | |
| Half Maximal Inhibitory Concentration (IC50) | 2 | nmol/L |
L-428 cells
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Hodgkin lymphoma
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[1] |
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
CAC10-CPT-LA [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.00 ng/mL
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High CD30 expression (CD30+++; 285,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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| In Vitro Model | Precursor T-cell acute lymphoblastic leukemia | ALCL cells | CVCL_A036 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.00 ng/mL
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High CD30 expression (CD30+++; 180,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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| In Vitro Model | Anaplastic large cell lymphoma | DEL/BVR cells | CVCL_1170 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 400,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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| In Vitro Model | Hodgkin's disease | L540cy cells | Homo sapiens | ||
| Experiment 4 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 320,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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|
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| In Vitro Model | ALK-positive anaplastic large cell lymphoma | Karpas-299 cells | CVCL_1324 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | Low CD30 expression (CD30+; 70,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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| In Vitro Model | Hodgkin lymphoma | L-428 cells | CVCL_1361 | ||
H00-CPT-LA [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 400,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
|
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| In Vitro Model | Hodgkin's disease | L540cy cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 320,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
|
||||
| In Vitro Model | ALK-positive anaplastic large cell lymphoma | Karpas-299 cells | CVCL_1324 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | Low CD30 expression (CD30+; 70,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
|
||||
| In Vitro Model | Hodgkin lymphoma | L-428 cells | CVCL_1361 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 285,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
|
||||
| In Vitro Model | Precursor T-cell acute lymphoblastic leukemia | ALCL cells | CVCL_A036 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 180,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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|
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| In Vitro Model | Anaplastic large cell lymphoma | DEL/BVR cells | CVCL_1170 | ||
References
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