GW583340
GW583340 is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW583340 exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW583340 is applicable to research related to head and neck cancer, breast cancer, and gastric cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 388082-81-3
- Fòrmula: C28H25ClFN5O3S2
- Peso molecular:598.11
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas EGFR
More
Actividad biológica
GW583340 (compound 6) potently inhibits purified EGFR and ErbB-2 tyrosine kinase activity in vitro cell-free assays, with an average dual enzyme inhibition IC50 of 0.012 μM[1].
GW583340 potently and selectively inhibits the proliferation of EGFR-overexpressing HN5, ErbB-2-overexpressing N87, and ErbB-2-overexpressing BT474 human tumor cell lines, with an average tumor cell IC50 of 0.11 μM and a selectivity ratio of >210-fold for tumor cells over normal HFF cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Bioavailability |
|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 39.5 % |
GW583340 (30-100 mg/kg; p.o.; twice daily; 21 days) produces 83% tumor inhibition in BT474 ErbB-2-overexpressing human breast carcinoma xenografts in female CD-1 mice, with no significant body weight loss observed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:CD-1 (female)[1]
-
Dosage:30; 100 mg/kg
-
Administration:p.o.; twice daily; 21 days
-
Result:Produced 81% tumor inhibition at 100 mg/kg.
Produced a lower level of tumor inhibition relative to the 100 mg/kg dose at 30 mg/kg.\nProduced 83% tumor inhibition at 100 mg/kg.
Produced a lower level of tumor inhibition relative to the 100 mg/kg dose at 30 mg/kg.
Showed no significant body weight loss in treated mice, indicating a good therapeutic index.
Chemical Information
-
No. CAS 388082-81-3
-
Peso molecular 598.11
-
Fòrmula C28H25ClFN5O3S2
-
SMILES
O=S(=O)(C)CCNCC1=NC(=CS1)C=2C=CC3=NC=NC(NC4=CC=C(OCC=5C=CC=C(F)C5)C(Cl)=C4)=C3C2
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GW583340 Related Classifications
HY-103439A Related Classifications
Powered by Bioz