Vandetanib (ZD6474)

Catalog No.: A10963

VEGFR inhibitor

Vandetanib (ZD6474)

Vandetanib (ZD6474) Chemical Structure

CAS NO. 443913-73-3

Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.

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25 mg

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50 mg

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100 mg

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500 mg

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  • Shinya Kitamura, .et al. Vandetanib inhibits cell growth in EGFR-expressing cutaneous squamous cell carcinoma, Biochem Biophys Res Commun, 2020, Aug 13 PMID: 32800552
  • Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
  • Park K, .et al. Vascular endothelial growth factor receptor 1 (VEGFR1) tyrosine kinase signaling facilitates granulation tissue formation with recruitment of VEGFR1+ cells from bone marrow, Anat Sci Int, 2018, Jun;93(3):372-383 PMID: 29256114
  • Rintaro Sogawa, .et al. Development of a competitive enzyme-linked immunosorbent assay for therapeutic drug monitoring of afatinib, JPA, 2018, in Press PMID: 30740257
  • Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
  • Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
  • Park K, .et al. Vascular endothelial growth factor receptor-1 (VEGFR-1) signaling enhances angiogenesis in a surgical sponge model, Biomed Pharmacother, 2016, Mar;78:140-149 PMID: 26898435

Biological Activity

Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
Targets
VEGFR2 (Cell-free assay)
40 nM
In vitro (25°C) DMSO 4 mg/mL (8.41 mM)
Water Insoluble
Ethanol Insoluble
In vivo 1% CMC Na 28 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 21.03 mL 105.17 mL 210.35 mL
0.5 mM 4.21 mL 21.03 mL 42.07 mL
1 mM 2.1 mL 10.52 mL 21.03 mL
5 mM 0.42 mL 2.1 mL 4.21 mL

*The above data is based on the productmolecular weight 475.4. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A10963
Actions Inhibitor
CAS No. 443913-73-3
Formula C22H24BrFN4O2
M. Wt 475.4
Purity >98%
Synonyms ZD6474
SMILES CN1CCC(CC1)COC2=C(C=C3C(=C2)N=CN=C3NC4=C(C=C(C=C4)Br)F)OC
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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