2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. Tyrosine Hydroxylase EGFR
  4. 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.

For research use only. We do not sell to patients.

GW583340

GW583340 Chemical Structure

CAS No. : 388082-81-3

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GW583340 Related Antibodies

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Description

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[1].

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.

GW583340 Related Antibodies
Parmacokinetics
Species Dose Route Bioavailability
Mice[1] 10 mg/kg p.o. 39.5 %
In Vivo

GW583340 (compound 6) (30-100 mg/kg; p.o.; twice daily; 21 days) produces 81% tumor inhibition in HN5 EGFR-overexpressing human head and neck carcinoma xenografts in female CD-1 mice[1].
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.
Molecular Weight

598.11

Formula

C28H25ClFN5O3S2
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GW583340 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GW583340388082-81-3GW 583340GW-583340Tyrosine HydroxylaseEGFRTyrH, THEpidermal growth factor receptorErbB-1HER1xenograft modelsHN5N87ErbB-2gastric carcinomatyrosine kinasehead and neck carcinomanormal human foreskin fibroblastsbreast carcinomaInhibitorinhibitorinhibit

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