General Information of This Payload
Payload ID
PAY0YCQYO
Name
Topo1 inhibitor D
Synonyms
Topo1 inhibitor D
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Target DNA topoisomerase I (TOP1)
Structure
Formula
C25H23N3O5
Isosmiles
CC[C@]1(O)C(C=C2C3=C(CN24)C(CN5C(CCC5)=O)=C6C=CC=CC6=N3)=C(COC1=O)C4=O
InChI
InChI=1S/C25H23N3O5/c1-2-25(32)18-10-20-22-16(12-28(20)23(30)17(18)13-33-24(25)31)15(11-27-9-5-8-21(27)29)14-6-3-4-7-19(14)26-22/h3-4,6-7,10,32H,2,5,8-9,11-13H2,1H3/t25-/m0/s1
InChIKey
TWQWSSOJWGYYLM-VWLOTQADSA-N
Pharmaceutical Properties
Molecule Weight
445.475
Polar area
101.73
Complexity
1391.786015
xlogp Value
2.202
Heavy Count
33
Rot Bonds
3
Hbond acc
7
Hbond Donor
1
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
CN112341521B+ADC-5 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC54)
20.44 ug/mL
Method Description
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (54%% inhibitory concentration).
In Vitro Model Lung adenocarcinoma HCC-827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC53)
1181 ug/mL
Method Description
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (53%% inhibitory concentration).
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC52)
64.44 ug/mL
Method Description
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (52%% inhibitory concentration).
In Vitro Model Lung adenocarcinoma NCI-H1650 cells CVCL_1483
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC51)
25.96 ug/mL
Method Description
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (51%% inhibitory concentration).
In Vitro Model Squamous cell carcinoma of the oral tongue, Tongue squamous cell carcinoma CAL33 cells CVCL_1108
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.69 ug/mL
Method Description
Add the antibody-coupled drug product C or nimotuzumab with a specified concentration to the cells, incubate for 3 days, and then add 40uL of Promega CellTiter-Glo reagent (Promega catalog number G968B). Subsequently, the chemiluminescence reading from CellTiter-Glo reagent was read to determine IC50 (50%% inhibitory concentration).
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
References
Ref 1 Small-molecule active compounds and their antibody conjugates, preparation methods and medical uses