Linker Information
General Information of This Linker
| Linker ID |
LIN0NIDLH
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
Maleimide-noncleavable-C6-linker
|
|||||
| Linker Type |
Uncleavable linker
|
|||||
| Antibody-Linker Relation |
Uncleavable
|
|||||
| Structure |
|
|||||
| Formula |
C10H17NO3
|
|||||
| Isosmiles |
OCCCCCCN1C(CCC1=O)=O
|
|||||
| PubChem CID | ||||||
| InChI |
InChI=1S/C10H17NO3/c12-8-4-2-1-3-7-11-9(13)5-6-10(11)14/h12H,1-8H2
|
|||||
| InChIKey |
BIKMYXBBCSSQLK-UHFFFAOYSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
199.25
|
Polar area
|
57.61
|
||
|
Complexity
|
184.08385
|
xlogp Value
|
0.6881
|
|||
|
Heavy Count
|
14
|
Rot Bonds
|
6
|
|||
|
Hbond acc
|
3
|
Hbond Donor
|
1
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
hRS7 ATAC 2 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.1 nM
|
Moderate TROP2 expression (TROP2++) | ||
| Method Description |
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.
Click to Show/Hide
|
||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-2 cells | CVCL_0026 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.2 nM
|
High TROP2 expression (TROP2 +++) | ||
| Method Description |
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.
Click to Show/Hide
|
||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.2 nM
|
High TROP2 expression (TROP2 +++) | ||
| Method Description |
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.
Click to Show/Hide
|
||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
138 nM
|
Moderate TROP2 expression (TROP2++) | ||
| Method Description |
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.
Click to Show/Hide
|
||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-2 cells | CVCL_0026 | ||
References