General Information of This Payload
Payload ID
PAY0JNJHU
Name
FDA026-LE21 payload
Synonyms
YSWPAY0017
   Click to Show/Hide
Structure
Formula
C30H33FN4O8S
Isosmiles
CC1=C(F)C=C2C3=C1CC[C@H](NC(CO)=O)C3=C(CN4C5=CC([C@](CC)(OCNCCS(C)(=O)=O)C6=O)=C(CO6)C4=O)C5=N2
InChI
InChI=1S/C30H33FN4O8S/c1-4-30(43-14-32-7-8-44(3,40)41)19-9-23-27-17(11-35(23)28(38)18(19)13-42-29(30)39)26-21(33-24(37)12-36)6-5-16-15(2)20(31)10-22(34-27)25(16)26/h9-10,21,32,36H,4-8,11-14H2,1-3H3,(H,33,37)/t21-,30-/m0/s1
InChIKey
YMIMHOQTRGIAKB-JRPXNJEYSA-N
Pharmaceutical Properties
Molecule Weight
628.679
Polar area
165.92
Complexity
1846.583405
xlogp Value
1.23892
Heavy Count
44
Rot Bonds
9
Hbond acc
11
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
FDA026-LE21 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
46.3 nM
Method Description
SK-BR-3 (ATCC) cells were selected as the cell line for in vitro activity detection experiments. 2000 cells were inoculated into each well of a 96-well cell culture plate and cultured for 20-24 hours. The antibody-drug conjugate prepared according to the method in Example 3 was formulated with L15 cell culture medium containing 10% FBS into 11 concentration gradients of test solution: 1000, 166.7, 55.6, 18.6, 6.17, 2.06, 0.69, 0.23, 0.08, 0.008 and OnM. 100 ul of the diluted test solution per well was added to the culture plate containing the inoculated cells and incubated in a 37°C, 5% CO, incubator for 144 hours. Then, CellTiter-Glo® Luminescent Cell Viability Assay Reagent (50 ul/well) was added, and the mixture was shaken at 500 rpm at room temperature for 10 minutes. The data were read using a SpectraMaxL microplate reader (OD570nm, with 2-second interval readings), and the IC50 results were calculated.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
89.34 nM
Method Description
NCI-H820 (ATCC) cells were selected as the cell line for in vitro activity detection experiments. 2000 cells were inoculated into each well of a 96-well cell culture plate and cultured for 20-24 hours. The antibody-drug conjugate prepared according to the method in Example 3 was formulated with L15 cell culture medium containing 10% FBS into 11 concentration gradients of test solution: 1000, 166.7, 55.6, 18.6, 6.17, 2.06, 0.69, 0.23, 0.08, 0.008 and OnM. 100 ul of the diluted test solution per well was added to the culture plate containing the inoculated cells and incubated in a 37°C, 5% CO, incubator for 144 hours. Then, CellTiter-Glo® Luminescent Cell Viability Assay Reagent (50 ul/well) was added, and the mixture was shaken at 500 rpm at room temperature for 10 minutes. The data were read using a SpectraMaxL microplate reader (OD570nm, with 2-second interval readings), and the IC50 results were calculated.

   Click to Show/Hide
In Vitro Model Lung papillary adenocarcinoma NCI-H820 cells CVCL_1592
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
98.26 nM
Method Description
22Rv1 (ATCC) cells were selected as the cell line for in vitro activity detection experiments. 2000 cells were inoculated into each well of a 96-well cell culture plate and cultured for 20-24 hours. The antibody-drug conjugate prepared according to the method in Example 3 was formulated with L15 cell culture medium containing 10% FBS into 11 concentration gradients of test solution: 1000, 166.7, 55.6, 18.6, 6.17, 2.06, 0.69, 0.23, 0.08, 0.008 and OnM. 100 ul of the diluted test solution per well was added to the culture plate containing the inoculated cells and incubated in a 37°C, 5% CO, incubator for 144 hours. Then, CellTiter-Glo® Luminescent Cell Viability Assay Reagent (50 ul/well) was added, and the mixture was shaken at 500 rpm at room temperature for 10 minutes. The data were read using a SpectraMaxL microplate reader (OD570nm, with 2-second interval readings), and the IC50 results were calculated.

   Click to Show/Hide
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
References
Ref 1 Antibody-drug conjugates, intermediates, preparation methods and uses