Payload Information
General Information of This Payload
| Payload ID | PAY0BDBBW |
|||||
|---|---|---|---|---|---|---|
| Name | Camptothecin derivative 095 |
|||||
| Synonyms |
camptothecin derivative 095
Click to Show/Hide
|
|||||
| Target | DNA topoisomerase I (TOP1) | |||||
| Formula | C23H19FN2O5 |
|||||
| Isosmiles | CC[C@@]1(O)C(C=C2C3=NC4=CC(F)=C(O)C5=C4C(CCC5)=C3CN62)=C(COC1=O)C6=O |
|||||
| InChI |
InChI=1S/C23H19FN2O5/c1-2-23(30)14-6-17-19-12(8-26(17)21(28)13(14)9-31-22(23)29)10-4-3-5-11-18(10)16(25-19)7-15(24)20(11)27/h6-7,27,30H,2-5,8-9H2,1H3/t23-/m1/s1
|
|||||
| InChIKey |
SPBBAORZGUMZLY-HSZRJFAPSA-N
|
|||||
| Pharmaceutical Properties | Molecule Weight |
422.412 |
Polar area |
101.65 |
||
Complexity |
1374.129539 |
xlogp Value |
2.413 |
|||
Heavy Count |
31 |
Rot Bonds |
1 |
|||
Hbond acc |
7 |
Hbond Donor |
2 |
|||
The activity data of This Payload
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
40285886 7300-LP1003 [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) |
32.17 nM
|
|||
| Method Description |
SHP-77 cells were grown in RPMI-1640 medium supplemented with 10% FBS and 1 ug/mL puromycin at 37 °C in a 5% CO2 incubator. SHP-77 cells were dissociated using TrypLETM Express Enzyme (Thermo Fisher Scientific, Waltham, MA, USA) and, after counting, the cells were resuspended in RPMI-1640 medium supplemented with 10% FBS at a density of 3 × 104 cells/mL. The cells were plated in 96-well plates and incubated at 37 °C for 24 h. ADCs and payloads were diluted separately and added to the 96-well cell culture plates containing cells, followed by incubation in a 5% CO2 incubator for 5 days. A multifunctional microplate reader was used, and the absorbance was measured at 450 nm with a reference wavelength of 630 nm. The IC50 values were calculated using GraphPad Prism 10.1.2 software.
Click to Show/Hide
|
||||
| In Vitro Model | Small cell lung carcinoma | SHP-77 cells | CVCL_1693 | ||
40285886 7300-LP2004 [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) |
39.74 nM
|
|||
| Method Description |
SHP-77 cells were grown in RPMI-1640 medium supplemented with 10% FBS and 1 ug/mL puromycin at 37 °C in a 5% CO2 incubator. SHP-77 cells were dissociated using TrypLETM Express Enzyme (Thermo Fisher Scientific, Waltham, MA, USA) and, after counting, the cells were resuspended in RPMI-1640 medium supplemented with 10% FBS at a density of 3 × 104 cells/mL. The cells were plated in 96-well plates and incubated at 37 °C for 24 h. ADCs and payloads were diluted separately and added to the 96-well cell culture plates containing cells, followed by incubation in a 5% CO2 incubator for 5 days. A multifunctional microplate reader was used, and the absorbance was measured at 450 nm with a reference wavelength of 630 nm. The IC50 values were calculated using GraphPad Prism 10.1.2 software.
Click to Show/Hide
|
||||
| In Vitro Model | Small cell lung carcinoma | SHP-77 cells | CVCL_1693 | ||
40285886 7300-LP3004 [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) |
186.6 nM
|
|||
| Method Description |
SHP-77 cells were grown in RPMI-1640 medium supplemented with 10% FBS and 1 ug/mL puromycin at 37 °C in a 5% CO2 incubator. SHP-77 cells were dissociated using TrypLETM Express Enzyme (Thermo Fisher Scientific, Waltham, MA, USA) and, after counting, the cells were resuspended in RPMI-1640 medium supplemented with 10% FBS at a density of 3 × 104 cells/mL. The cells were plated in 96-well plates and incubated at 37 °C for 24 h. ADCs and payloads were diluted separately and added to the 96-well cell culture plates containing cells, followed by incubation in a 5% CO2 incubator for 5 days. A multifunctional microplate reader was used, and the absorbance was measured at 450 nm with a reference wavelength of 630 nm. The IC50 values were calculated using GraphPad Prism 10.1.2 software.
Click to Show/Hide
|
||||
| In Vitro Model | Small cell lung carcinoma | SHP-77 cells | CVCL_1693 | ||
References
