Dovitinib, class III-V receptor tyrosine kinase inhibitor (ab216312)

Overview

  • Product name

    Dovitinib, class III-V receptor tyrosine kinase inhibitor
  • Description

    Potent, selective class III-V receptor tyrosine kinase inhibitor
  • Alternative names

    • CHIR258
    • TKI-258
  • Biological description

    Potent, selective inhibitor of class III-V receptor tyrosine kinases (RTKs). Inhibits FLT3 (IC50 = 1 nM), c-KIT (IC50 = 2 nM), FGFR (IC50 = 8 nM), VEGFR1/2/3 (IC50 values are 10 nM, 13 nM and 8 nM respectively), PDGFRβ (IC50 = 27 nM), and CSF-1R (IC50 = 36 nM). Selectively blocks growth of B9 cells transformed by wild type, or activated mutant FGFR3. Induces apoptosis, or sensitizes cells to induction of apoptosis by other means in a variety of cancer cell lines.

  • Purity

    > 99%
  • CAS Number

    405169-16-6
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one
  • Molecular weight

    392.43
  • Molecular formula

    C21H21FN6O
  • PubChem identifier

    9886808
  • Storage instructions

    Shipped at Room Temperature. Store at -20°C long term. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO (up to 30 mg/ml)

  • SMILES

    CN1CCN(CC1)c2cc3nc(nc3cc2)C4=C(N)c5c(F)cccc5NC4=O
  • Source

    TLC and HPLC

References

This product has been referenced in:

  • Tai WT  et al. Dovitinib induces apoptosis and overcomes sorafenib resistance in hepatocellular carcinoma through SHP-1-mediated inhibition of STAT3. Mol Cancer Ther 11:452-63 (2012). Read more (PubMed: 22180308) »
  • Xin X  et al. CHIR-258 is efficacious in a newly developed fibroblast growth factor receptor 3-expressing orthotopic multiple myeloma model in mice. Clin Cancer Res 12:4908-15 (2006). Read more (PubMed: 16914579) »
  • Trudel S  et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood 105:2941-8 (2005). Read more (PubMed: 15598814) »
  • Lee SH  et al. In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models. Clin Cancer Res 11:3633-41 (2005). Read more (PubMed: 15897558) »

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