Linker Information
General Information of This Linker
| Linker ID |
LIN0BEGYO
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| Linker Name |
Open-chain glycine maleimide-PEG
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| Linker Type |
Flexible reactive (thiol) linker
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| Antibody-Linker Relation |
Uncleavable
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| Structure |
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| Formula |
C26H45N3O13
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| Isosmiles |
COCCOCCOCCOCCOCCOCCC(=O)NCCCCC(NC(=O)CNC(=O)/C=C/C(=O)O)C(=O)O
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| InChI |
InChI=1S/C26H45N3O13/c1-37-10-11-39-14-15-41-18-19-42-17-16-40-13-12-38-9-7-23(31)27-8-3-2-4-21(26(35)36)29-24(32)20-28-22(30)5-6-25(33)34/h5-6,21H,2-4,7-20H2,1H3,(H,27,31)(H,28,30)(H,29,32)(H,33,34)(H,35,36)/b6-5+
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| InChIKey |
OZYYGPJZDXELER-AATRIKPKSA-N
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| Pharmaceutical Properties |
Molecule Weight
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607.654
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Polar area
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217.28
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Complexity
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42
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xlogp Value
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-1.2812
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Heavy Count
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42
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Rot Bonds
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29
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Hbond acc
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11
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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
HER2-EC5 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
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High CD276 expression (CD276+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
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High LYPD3 expression (LYPD3+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
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| In Vitro Model | Lung adenocarcinoma | A549-C4.4a cells | CVCL_0023 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 uM | High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
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| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
C4.4A-EC5 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
8.40 nM
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High LYPD3 expression (LYPD3+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
Click to Show/Hide
|
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| In Vitro Model | Lung adenocarcinoma | A549-C4.4a cells | CVCL_0023 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
48.00 nM
|
High CD276 expression (CD276+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
Click to Show/Hide
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 uM | High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
Click to Show/Hide
|
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| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
B7H3-EC5 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 uM | High CD276 expression (CD276+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
Click to Show/Hide
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 uM | High LYPD3 expression (LYPD3+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
Click to Show/Hide
|
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| In Vitro Model | Lung adenocarcinoma | A549-C4.4a cells | CVCL_0023 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 uM | High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++) | ||
| Method Description |
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.
Click to Show/Hide
|
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| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
References
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