Linker Information
General Information of This Linker
| Linker ID |
LIN0VQWJS
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| Linker Name |
aHer2- (AL7-LP5)<sub>3.80</sub> 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 |
C49H82N10O15
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| Isosmiles |
O=C(C)NCCOCCOCCOCCN(N=N1)C2=C1C(OCC(NCCOCCOCCOCCOCCC(N[C@H](C(N[C@@H](CCCNC(N)=O)C(NC3=CC=C(CO)C=C3)=O)=O)C(C)C)=O)=O)CCCCC2
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| InChI |
InChI=1S/C49H82N10O15/c1-36(2)45(48(65)55-40(8-7-16-53-49(50)66)47(64)54-39-13-11-38(34-60)12-14-39)56-43(62)15-20-67-24-28-71-32-33-73-30-26-69-22-18-52-44(63)35-74-42-10-6-4-5-9-41-46(42)57-58-59(41)19-23-70-27-31-72-29-25-68-21-17-51-37(3)61/h11-14,36,40,42,45,60H,4-10,15-35H2,1-3H3,(H,51,61)(H,52,63)(H,54,64)(H,55,65)(H,56,62)(H3,50,53,66)/t40-,42?,45-/m0/s1
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| InChIKey |
CJNKBHVZAOBPFE-SONZDUBQSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1051.25
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Polar area
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325.4
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Complexity
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1816.441824
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xlogp Value
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0.416
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Heavy Count
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74
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Rot Bonds
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41
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Hbond acc
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18
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Hbond Donor
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8
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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
aHer2- (AL7-LP5)3.80 [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) |
0.216 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well SK-BR-3 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.327 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well Calu-3 in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.
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| In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
2.19 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well NCI-N87 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.
Click to Show/Hide
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 400 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 800/well NCI-H1975 cells in 80ul media (target negative cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.
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| In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
FelD1- (AL7-LP5)3.69 [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) |
178 nM
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Positive HER2expression (HER2+++/++) | ||
| Method Description |
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well Calu-3 in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.
Click to Show/Hide
|
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| In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
204 nM
|
Positive HER2expression (HER2+++/++) | ||
| Method Description |
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well SK-BR-3 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.
Click to Show/Hide
|
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
400 nM
|
Positive HER2expression (HER2+++/++) | ||
| Method Description |
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well NCI-N87 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.
Click to Show/Hide
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 400 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 800/well NCI-H1975 cells in 80ul media (target negative cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.
Click to Show/Hide
|
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| In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
References