GW837016X
GW837016X (NEU-391) is an orally active ErbB-2 kinase covalent inhibitor. GW837016X also is a potent antitrypanosome agent. GW837016X inhibits mitosis and cytokinesis.
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- CAS No.: 833473-68-0
- Formule: C25H20ClFN4OS
- Masse moléculaire:478.97
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[1]|
ErbB2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | IC50 |
205 nM
Compound: 7
|
Antiproliferative activity against human BT474 cells overexpressing ErbB2 after 3 days by methylene blue staining
Antiproliferative activity against human BT474 cells overexpressing ErbB2 after 3 days by methylene blue staining
|
[PMID: 18842405] |
| Fibroblast | IC50 |
>1 μM
Compound: 7
|
Antiproliferative activity against human foreskin fibroblast after 3 days by methylene blue staining
Antiproliferative activity against human foreskin fibroblast after 3 days by methylene blue staining
|
[PMID: 18842405] |
| HN5 | IC50 |
536 nM
Compound: 7
|
Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining
Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining
|
[PMID: 18842405] |
In Vitro
GW837016X inhibits proliferation of bloodstream Trypanosoma brucei with an IC50 value of 0.4 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Swiss Webster mice (T. brucei (Lister427)) [1]
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Dosage:130 mg/kg
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Administration:P.o.; daily for 10 days
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Result:Increased the mean survival and inhibited Trypanosoma brucei proliferation.
Chemical Information
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CAS No. 833473-68-0
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Masse moléculaire 478.97
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Formule C25H20ClFN4OS
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SMILES
FC1=CC(COC2=CC=C(NC3=C4C(C=C(C#C[C@H]5NCCC5)S4)=NC=N3)C=C2Cl)=CC=C1
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Synonyms
NEU-391
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)