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Gefitinib HCl

Cat. No. M5679

Gefitinib HCl Structure
Size Price Availability Quantity
100mg USD 100 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Gefitinib Hcl(ZD-1839 Hcl) is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 483.36
Formula C22H25Cl2FN4O3
CAS Number 184475-55-6
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Sci Rep (2017). Figure 7. Gefitinib (AbMole Bioscience, Houston, TX)
Method TKI gefitinib inhibits RIPK2-mediated dysglycemia in vivo.
Cell Lines C57Bl/6J (WT) and RIPK2−/− mice
Concentrations 100 mg/kg
Incubation Time 4 days
Results Pre-treatment with gefitinib attenuated lower blood glucose at 6 h post-FK565 injection. At the time of the glucose tolerance test (GTT, 24 h after FK565 injection) gefitinib pre-treatment did not alter fasting blood glucose.
Rating
Source Sci Rep (2017). Figure 6. Gefitinib (AbMole Bioscience, Houston, TX)
Method TKI gefitinib inhibits RIPK2-mediated inflammation in vivo.
Cell Lines RIPK2−/− mice
Concentrations 5–200 mg/kg
Incubation Time 4 days
Results Our results show that treatment with gefitinib at doses equal or greater than 50 mg/kg attenuated Nod1 mediated Cxcl1 protein levels in the circulation of mice in a dose-dependent manner.
Rating
Source Sci Rep (2017). Figure 5. Gefitinib (AbMole Bioscience, Houston, TX)
Method C57Bl/6J (WT) and RIPK2−/− mice
Cell Lines HEK293 cells
Concentrations 1 or 5 μM
Incubation Time
Results We assessed FK565- versus LPS-induced NF-κB activity using HEK293 cells stably over-expressing Nod1 or Tlr4. Consistent with cytokine secretion in adipocytes and macrophages, we find that treatment of HEK Nod1 cells with FK565 (10 μg/mL) increases NF-κB activation, which is attenuated in a dose-dependent manner by pre-incubation with gefitinib at 1 and 5 μM.
Rating
Source Sci Rep (2017). Figure 4. Gefitinib (AbMole Bioscience, Houston, TX)
Method
Cell Lines bacterial cell
Concentrations 0.2, 1 or 5 μM
Incubation Time 1 h
Results Time course of FK565-stimulated Cxcl1 secretion in BMDMs (B) n = 4–12. Levels of Cxcl1 released from WT (left panel) or RIPK2−/−(right panel) BMDMs after stimulation with the Tlr4 ligand LPS (0.5 μg/mL) for 48 h and pre-incubated for 1 h with 0.2, 1 or 5 μM gefitinib or SB203580 (C) n = 4–12.
Rating
Source Sci Rep (2017). Figure 3. Gefitinib (AbMole Bioscience, Houston, TX)
Method Westen Blot
Cell Lines bacterial cell
Concentrations 5 μM
Incubation Time 1 h
Results Quantitative comparison was conducted between samples from 4 different blots derived from the same experiment and processed in parallel. (n = 8 total (n = 2/condition per blot).
Rating
Source Sci Rep (2017). Figure 2. Gefitinib (AbMole Bioscience, Houston, TX)
Method TKIs inhibit cytokine response
Cell Lines bacterial cell
Concentrations 1 or 5 μM
Incubation Time 1 h
Results Our results show that pre-incubation with 1–5 μM gefitinib or 1–5 μM SB203580, but not 1–5 μM imatinib significantly attenuated FK565-induced Cxcl1 and Il6 release in a dose-dependent manner in adipocytes.
Rating
Source Sci Rep (2017). Figure 1. Gefitinib (AbMole Bioscience, Houston, TX)
Method bacterial cell wall-induced lipolysis
Cell Lines Murine 3T3-L1 preadipocytes
Concentrations 5 μM
Incubation Time 48 h
Results Only 1 or 5 μM gefitinib and 1 or 5 μM SB203580 dose dependently attenuated the increased rate of glycerol release induced by FK565.
Rating
Product Citations
References

Gefitinib and erlotinib in metastatic non-small cell lung cancer: a meta-analysis of toxicity and efficacy of randomized clinical trials.
Burotto M, et al. Oncologist. 2015 Apr;20(4):400-10. PMID: 25795635.

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  Catalog
Abmole Inhibitor Catalog 2017




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