Payload Information
General Information of This Payload
| Payload ID | PAY0FNIZI |
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|---|---|---|---|---|---|---|
| Name | Neolymphostin A |
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| Synonyms |
CHEMBL4293970; neolymphostin A; GTPL10151; BDBM50468033; NSC790970; compound 4 [PMID: 30380865]; NSC-790970
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| Target(s) | 3-Phosphoinositide-dependent protein kinase 1 (PDPK1) | |||||
| Structure |
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| Formula | C18H18N4O3 |
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| Isosmiles | CC(C)C(=O)NC1=CC(=N)C2=NC=C3C2=C1NC(=C3)C(=O)/C=C/OC |
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| PubChem CID | ||||||
| InChI |
InChI=1S/C18H18N4O3/c1-9(2)18(24)22-13-7-11(19)16-15-10(8-20-16)6-12(21-17(13)15)14(23)4-5-25-3/h4-9,19,21H,1-3H3,(H,22,24)/b5-4+,19-11?
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| InChIKey |
AMBGZHQTMCPRDB-SSQJTDSESA-N
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| IUPAC Name |
N-[11-imino-6-[(E)-3-methoxyprop-2-enoyl]-2,7-diazatricyclo[6.3.1.04,12]dodeca-1,3,5,8(12),9-pentaen-9-yl]-2-methylpropanamide
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| Pharmaceutical Properties | Molecule Weight |
338.4 |
Polar area |
108 |
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Complexity |
640 |
xlogp Value |
1.3 |
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Heavy Count |
25 |
Rot Bonds |
5 |
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Hbond acc |
5 |
Hbond Donor |
3 |
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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
Neolymphostin ADC 21 [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) |
77.30 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
225 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Neolymphostin ADC 23 [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) |
152 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
274 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
386 nM
|
High HER2 expression (HER2+++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
|
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Neolymphostin ADC 24 [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) |
195 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
202 nM
|
High HER2 expression (HER2+++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
216 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 750 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Neolymphostin ADC 22 [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) |
251 nM
|
High HER2 expression (HER2+++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
|
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
423 nM
|
High HER2 expression (HER2+++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
|
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2++) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
References
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