General Information of This Payload
Payload ID
PAY0BDBBW
Name
Camptothecin derivative 095
Synonyms
camptothecin derivative 095
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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
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 14.39 nM
SHP-77 cells
Small cell lung carcinoma
CVCL_1693 
[1]
Half Maximal Inhibitory Concentration (IC50) 14.39 nM
SHP-77 cells
Small cell lung carcinoma
CVCL_1693 
[1]
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
Click To Hide/Show 1 Activity Data Related to This Level
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.

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In Vitro Model Small cell lung carcinoma SHP-77 cells CVCL_1693
40285886 7300-LP2004 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
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
Click To Hide/Show 1 Activity Data Related to This Level
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
Ref 1 Design, Synthesis, and Evaluation of Camptothecin-Based Antibody-Drug Conjugates with High Hydrophilicity and Structural Stability