Linker Information
General Information of This Linker
| Linker ID |
LIN0DWRJM
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| Linker Name |
FDA026-LE20 linker
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C47H74N8O15
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| Isosmiles |
C[C@H](NC([C@@H](NC(CCOCCOCCOCCOCCOCCOCCOCCOCCN1N=NC(CNC(CCCCCN2C(C=CC2=O)=O)=O)=C1)=O)C(C)C)=O)C(NC3=CC=C(CO)C=C3)=O
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| InChI |
InChI=1S/C47H74N8O15/c1-36(2)45(47(62)49-37(3)46(61)50-39-10-8-38(35-56)9-11-39)51-42(58)14-17-63-19-21-65-23-25-67-27-29-69-31-32-70-30-28-68-26-24-66-22-20-64-18-16-54-34-40(52-53-54)33-48-41(57)7-5-4-6-15-55-43(59)12-13-44(55)60/h8-13,34,36-37,45,56H,4-7,14-33,35H2,1-3H3,(H,48,57)(H,49,62)(H,50,61)(H,51,58)/t37-,45-/m0/s1
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| InChIKey |
ZRZPABLFLAFJSX-JJXMVLQZSA-N
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| Pharmaceutical Properties |
Molecule Weight
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991.15
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Polar area
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278.56
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Complexity
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1745.249805
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xlogp Value
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0.6791
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Heavy Count
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70
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Rot Bonds
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42
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Hbond acc
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18
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Hbond Donor
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5
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
FDA026-LE20 [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) |
46.15 nM
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| 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.
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| 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) |
52.33 nM
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| Method Description |
SW620 (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 IC58 results were calculated.
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| In Vitro Model | Colon adenocarcinoma | SW620 cells | CVCL_0547 | ||