Dovitinib

• Description:

  Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity[1][2].

• Product Name Alternative:

  CHIR-258; TKI258

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  C-Fms; c-Kit; FGFR; FLT3; PDGFR; VEGFR

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Dovitinib.html

• Purity:

  99.88

• Solubility:

  DMSO : 23.33 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles:

  O=C1NC (C=CC=C2F) =C2C (N) =C1C3=NC4=CC=C (N5CCN (C) CC5) C=C4N3

• Molecular Formula:

  C21H21FN6O

• Molecular Weight:

  392.43

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t (4;14) multiple myeloma. Blood. 2005, 105 (7), 2941-2948.|[2]Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56 (3), 595-601.|[3]Lee Y, et al. A Receptor Tyrosine Kinase Inhibitor, Dovitinib (TKI-258), Enhances BMP-2-Induced Osteoblast Differentiation In Vitro. Mol Cells. 2016 May 31;39 (5) :389-94|[4]Chon HJ, et al. Traf2- and Nck-interacting kinase (TNIK) is involved in the anti-cancer mechanism of dovitinib in human multiple myeloma IM-9 cells. Amino Acids. 2016 Jul;48 (7) :1591-9.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 3

• Isoform:

  PDGFRα; PDGFRβ; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

• Citation 01:

  Biochemistry for Health, NOVA University of Lisbon. 2019 Jul.|bioRxiv. 2024 June 09.|Front Cell Dev Biol. 2020 May 7:8:287.|Harvard Medical School LINCS LIBRARY|J Biol Chem. 2023 Apr;299 (4) :104595|NPJ Precis Oncol. 2021 Jul 16;5 (1) :66.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Theranostics. 2018 Jul 30;8 (15) :4262-4278.|University of Düsseldorf. 2024.|Nat Commun. 2025 Jul 24;16 (1) :6777.

• CAS Number:

  405169-16-6