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.
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- CAS No.: 388082-81-3
- 화학식: C28H25ClFN5O3S2
- 분자량:598.11
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보관:
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]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
In Vitro
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.
Parmacokinetics
| Species | Dose | Route | Bioavailability |
|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 39.5 % |
In Vivo
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.
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Animal Model:CD-1 (female)[1]
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Dosage:30; 100 mg/kg
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Administration:p.o.; twice daily; 21 days
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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
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CAS No. 388082-81-3
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분자량 598.11
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화학식 C28H25ClFN5O3S2
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GW583340 Related Classifications
HY-103439A Related Classifications
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