Linker Information
General Information of This Linker
| Linker ID |
LIN0EPGVZ
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| Linker Name |
FDA026-LE19 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 |
C32H44N8O7
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| Isosmiles |
C[C@H](NC([C@@H](NC(CCCN1N=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/C32H44N8O7/c1-21(2)30(32(47)34-22(3)31(46)35-24-12-10-23(20-41)11-13-24)36-27(43)9-7-16-39-19-25(37-38-39)18-33-26(42)8-5-4-6-17-40-28(44)14-15-29(40)45/h10-15,19,21-22,30,41H,4-9,16-18,20H2,1-3H3,(H,33,42)(H,34,47)(H,35,46)(H,36,43)/t22-,30-/m0/s1
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| InChIKey |
ZCJLPYVSUNYIOH-CHJDUVSTSA-N
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| Pharmaceutical Properties |
Molecule Weight
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652.753
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Polar area
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204.72
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Complexity
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1361.61835
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xlogp Value
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0.9364
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Heavy Count
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47
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Rot Bonds
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19
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Hbond acc
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10
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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-LE19 [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) |
40.28 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 IC57 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) |
52.38 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 | ||