Payload Information
General Information of This Payload
| Payload ID | PAY0SIOMR |
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| Name | aHer2- (AL7-LP5D)<sub>3.89</sub> Payload |
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| Synonyms |
aHer2- (AL7-LP5D)<sub>3.89</sub> Payload
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| Structure |
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| Formula | C33H41FN6O7 |
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| Isosmiles | NCCCC[C@@H](C(NCOCC(N[C@H](/C=C1CN(C(C\1=N\2)=C3)C(C(CO4)=C3[C@@](O)(CC)C4=O)=O)CCC5=CC2=CC(F)=C5C)=O)=O)N |
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| InChI |
InChI=1S/C33H41FN6O7/c1-3-33(45)24-13-27-29-20(14-40(27)31(43)23(24)15-47-32(33)44)11-21(8-7-19-10-22(39-29)12-25(34)18(19)2)38-28(41)16-46-17-37-30(42)26(36)6-4-5-9-35/h10-13,21,26,45H,3-9,14-17,35-36H2,1-2H3,(H,37,42)(H,38,41)/t21-,26-,33-/m0/s1
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| InChIKey |
ODKZBWYBZMVCCJ-BNZLNIKKSA-N
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| Pharmaceutical Properties | Molecule Weight |
652.724 |
Polar area |
200.36 |
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Complexity |
1643.477525 |
xlogp Value |
0.98862 |
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Heavy Count |
47 |
Rot Bonds |
11 |
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Hbond acc |
11 |
Hbond Donor |
5 |
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Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
aHer2- (AL7-LP5D)3.89 [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) |
0.139 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) |
0.19 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 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) |
1.46 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.
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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) |
209 nM
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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 | ||
aHer2- (AL7-LP5D)3.90 [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) |
88.2 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.
Click to Show/Hide
|
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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) |
95.3 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.
Click to Show/Hide
|
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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) | > 169 nM | 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) |
280 nM
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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 | ||
References