Linker Information
General Information of This Linker
| Linker ID |
LIN0LWEJI
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| Linker Name |
FDA026-LE18 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 |
C33H46N8O6
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| Isosmiles |
C[C@H](NC([C@@H](NC(CCCN1N=NC(CNC(CC2)CCC2CN3C(C=CC3=O)=O)=C1)=O)C(C)C)=O)C(NC4=CC=C(CO)C=C4)=O
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| InChI |
InChI=1S/C33H46N8O6/c1-21(2)31(33(47)35-22(3)32(46)36-26-12-8-24(20-42)9-13-26)37-28(43)5-4-16-40-19-27(38-39-40)17-34-25-10-6-23(7-11-25)18-41-29(44)14-15-30(41)45/h8-9,12-15,19,21-23,25,31,34,42H,4-7,10-11,16-18,20H2,1-3H3,(H,35,47)(H,36,46)(H,37,43)/t22-,23?,25?,31-/m0/s1
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| InChIKey |
GSJQHMCHCFEVNA-UTGYMFEKSA-N
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| Pharmaceutical Properties |
Molecule Weight
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650.781
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Polar area
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187.65
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Complexity
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1357.61835
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xlogp Value
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1.4082
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Heavy Count
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47
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Rot Bonds
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16
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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-LE18 [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) |
41.69 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 IC56 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) |
45.32 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 | ||