Linker Information
General Information of This Linker
| Linker ID |
LIN0AAQNQ
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| Linker Name |
FDA026-LE15 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 |
C25H34N4O9S
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| Isosmiles |
C[C@H](NC([C@@H](NC(C(S(=O)(O)=O)CCCCN1C(C=CC1=O)=O)=O)C(C)C)=O)C(NC2=CC=C(CO)C=C2)=O
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| InChI |
InChI=1S/C25H34N4O9S/c1-15(2)22(25(35)26-16(3)23(33)27-18-9-7-17(14-30)8-10-18)28-24(34)19(39(36,37)38)6-4-5-13-29-20(31)11-12-21(29)32/h7-12,15-16,19,22,30H,4-6,13-14H2,1-3H3,(H,26,35)(H,27,33)(H,28,34)(H,36,37,38)/t16-,19?,22-/m0/s1
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| InChIKey |
UFQWDCRASQWYSQ-WFSJFSNBSA-N
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| Pharmaceutical Properties |
Molecule Weight
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566.633
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Polar area
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199.28
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Complexity
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1140.897312
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xlogp Value
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0.1146
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Heavy Count
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39
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Rot Bonds
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14
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Hbond acc
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8
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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-LE15 [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) |
47.86 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 IC53 results were calculated.
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| In Vitro Model | Colon adenocarcinoma | SW620 cells | CVCL_0547 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
53.12 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 | ||